Documenti di Didattica
Documenti di Professioni
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(INCLUDING IONOTROPES)
ANTICONVULSANT:
Barbiturates- Phenobarbitone
Deoxy Barbiturates-Primidone
Hydantoins- Phenytoin
Iminostilbens carbamazepine.
Valproic Acid- Sodium Valproate
Succinamides-Ethosuccinamide
Benzodiazepine-Clonazepam
-Carbamazepine
2
ANTIHYPERTENSIVES
Centrally Acting-Clonidine
Peripherally Acting-Prazosin
Beta Blockers-Atenolol
and blockers-labetalol
Acting on smooth muscle- sodium
nitroprusside
Calcium channel blockers- amlodipine
ACE inhibitors Enalapril
Antiogentsin II receptor antagonist- valsartan.
4
ANTI ANGINALS
Nitrates- isosorbide dinitrate
Beta adrenergic and calcium channel
blockers.
Antiplatelets- aspirin
Vasodialtion- cinnirazine
COAGULANTS
Vitamin k analogues
5
DIURETICS
Thiazide- hydrochlorthiazide
Loop- frusemide
Potassium sparing- spirinolactone
Carbonc anhydrase inibitors- acetazolamide
Osmotic diuretics- mannitol
ANAESTHETIC AGENTS:
Xylocaine
Propofol
OTHERS;
Morphine
Pethidine
Fentanyl.
(ADENOCARD), ADENOJET:
PHARMACOLOGICAL NAME: adenosine
INDICATION:
paroxysmal supraventricular tachycardia (PSVT).
DOSAGE AND ADMINISTRATION:
For rapid bolus intravenous use only.
Adult Patients-Initial dose: 6 mg given as a rapid
intravenous bolus (administered over a 1-2 second
period).
Repeat administration: If the first dose does not
result in elimination of the supraventricular
tachycardia within 1-2 minutes, 12 mg should be
given as a rapid intravenous bolus. This 12 mg dose
may be repeated a second time if required.
9
DOSAGE
SIDE EFFECTS:
Central Nervous System -Light headedness(2%),
dizziness, tingling in arms, numbness (1%),
apprehension, blurred vision, burning sensation,
heaviness in arms, neck and back pain (less than 1%).
Gastrointestinal Nausea (3%), metallic taste,
tightness in throat, pressure in groin (less than 1%).
Cardiovascular -Prolonged asystole, ventricular
tachycardia, ventricular fibrillation, transient increase
in blood pressure, bradycardia, atrial fibrillation
Respiratory -Bronchospasm
Central Nervous System -Seizure activity, including
tonic clonic (grand mal) seizures, and loss of
consciousness.
11
DRUG INTERACTIONS:
INHIBITED BY:caffeine and theophylline
POTENTIATED BY: dipyridamole.
OVERDOSE:
The half-life of Adenocard (adenosine injection) is less
than 10 seconds. Thus, adverse effects are generally
rapidly self-limiting.
CONTRAINDICATIONS
Second- or third-degree A-V block
Sinus node disease, such as sick sinus syndrome or
symptomatic bradycardia
Known hypersensitivity to adenosine.
MECHANISM OF ACTION
Hemodynamics
Adenosine decreases blood pressure by decreasing
peripheral resistance.
12
AMIODARONE:
GENERIC NAME: amiodarone BRAND NAME:
Cordarone
DRUG CLASS AND MECHANISM:
a slowing of the speed of electrical conduction
a reduction in the rapidity of firing (the heart's
pacemaker);
slowing of conduction through various
specialized electrical pathways (called accessory
pathways)
amiodarone also causes blood vessels to dilate
(enlarge). This effect can result in a drop in blood
pressure.
PREPARATIONS: Tablets (pink), round in shape:
200 mg.
13
STORAGE: Tablets should be kept at room
INDICATIONS:
ventricular fibrillation,
ventricular tachycardia,
atrial fibrillation, and
atrial flutter.
DRUG INTERACTIONS: Amiodarone may
interact with beta-blockers or calcium channel
blockers resulting in an excessively slow heart
rate or a block in the conduction of the electrical
impulse through the heart.
Amiodarone increases the blood levels of digoxin,
Procainamide and quinidine concentrations
increase by 30%-50% during the first week of
amiodarone therapy.
SIDE EFFECTS
14
INDICATIONS
1. As an antisialagogue
2. To blunt the increased vagal tone (decreased pulse and
blood pressure)
3. To temporarily increase heart rate or decrease AV-block until
definitive intervention can take place,
4. As an antidote for inadvertent overdose of cholinergic drugs
or for cholinesterase poisoning such as from organophosphorus
insecticides
5. As an antidote for the "rapid type of mushroom poisoning
due to the presence of the alkaloid muscarine
6. for reversal of neuromuscular blockade
DOSAGE AND ADMINISTRATION:
Adults
0.5 mg to 1 mg for antisialagogue and other antivagal effects,
2 to 3 mg as an antidote for organophosporous or muscarinic
mushroom poisoning.
Endotracheal administration of atropine -1 to 2 mg diluted to a
total not to exceed 10 ml of sterile water or normal saline.
16
Pediatrics
range of 0.01to 0.03 mg/kg body weight.
Store at controlled room temperature 15 to 30C (59 to 86F).
SIDE EFFECTS
Dryness of the mouth, blurred vision, photophobia and
tachycardia commonly occur with chronic administration of
therapeutic doses.
Constipation and difficulty in micturition may occur in elderly
patients. Occasional hypersensitivity reactions.
WARNINGS
Children are more susceptible than adults to the toxic effects of
anticholinergic agents.
Atropine is not removed by dialysis.
PRECAUTIONS
Do not administer unless solution is clear and seal is intact.
Discard unused portion.
acute glaucoma in susceptible patients
17
CONTRAINDICATIONS:
glaucoma, pyloric stenosis or prostatic hypertrophy,
except in doses ordinarily used for preanesthetic
medication.
CLINICAL PHARMACOLOGY
Atropine is commonly classified as an anticholinergic
or ant parasympathetic drug. Atropine inhibits the
muscarinic actions of acetylcholine on structures .
the major action of atropine is a competitive or
surmountable antagonism which can be overcome by
increasing the concentration of acetylcholine at
receptor sites of the effector organ (e.g., by using
anticholinesterase agents which inhibit the
enzymatic destruction of acetylcholine).
18
CALCIUM CHLORIDE:
CALCIUMCHLORIDE
Injection, 100 mg/mL(13.6 mEq Calcium/10 mL)
INDICATIONS
hypocalcemic tetany.
Insect bites or stings, such as Black Widow Spider bites.
Sensitivity reactions, particularly when characterized by urticaria.
treatment of depression due to over dosage of magnesium sulfate.
In cardiac resuscitation, particularly after open heart surgery,
DOSAGE AND ADMINISTRATION
The usual adult dose of this preparation varies from 5 to 10 mL at intervals
of 1 to 3 days.
In cardiac resuscitation, the usual dose is 2 to 4 mL injected into the
ventricular cavity.
19
WARNINGS
This solution is suitable only for intravenous use.
This product contains aluminum that may be toxic.
PRECAUTIONS
a digitalized patient should not receive an intravenous
injection of a calcium compound unless the indications are
clearly defined.
OVERDOSE:
The syndrome is characterized by weakness, lethargy,
intractable nausea and vomiting, coma, and sudden death,
and a markedly elevated plasma calcium level.
STORAGE:
Store at controlled room temperature 15-30C (59-86F)
CONTRAINDICATIONS
In cardiac resuscitation, the use of calcium chloride is
contraindicated in the presence of ventricular fibrillation.
20
CLINICAL PHARMACOLOGY:
Calcium is the fifth most abundant
element in the body; the major fraction is
in bone. It is essential for the functional
integrity of the nervous and muscular
systems, for normal cardiac contractility
and the coagulation of blood. It also
functions as an enzyme cofactor and
affects the secretory activity of endocrine
and exocrine glands.
DOPAMINE (HYDROCHLORIDE) Injection.
INDICATIONS
DOPAMINE is indicated for the correction of hemodynamic imbalances
present in the shock syndrome
restoration of blood volume
Poor Perfusion of Vital Organs:
Low Cardiac Output:
Hypotension:
WARNING: This is a potent drug: It must be diluted before administration to
patient.
Suggested Dilution: Transfer contents of one or more ampules or vials by
aseptic technique to either 250 mL or 500 mL of one of the following sterile
intravenous solutions:
Sodium Chloride Injection, USP
Dextrose (5%) Injection, USP
Dextrose (5%) and Sodium Chloride (0.9%) Injection, USP
5% Dextrose in 0.45% Sodium Chloride Solution
Lactated Ringer's Solution
Sodium Lactate (1/6 Molar) Injection, USP
22
23
SIDE EFFECTS
Cardiovascular System
ventricular arrhythmia (at very high doses
,ectopic beats ,tachycardia, anginal pain
,palpitation, cardiac conduction abnormalities,
widened QRS
complex,bradycardia,hypotension,hypertension
vasoconstriction
Respiratory System -dyspnea
Gastrointestinal System-nausea ,vomiting,
metabolic/Nutritional System, azotemia
Central Nervous System-headache, anxiety
Dermatological System- piloerection
Other
Gangrene of the extremities
24
DRUG INTERACTIONS
Therefore, EXTREME CAUTION should be exercised
when administering dopamine HCl to patients receiving
cyclopropane or halogenated hydrocarbon anaesthetics.
WARNINGS
Do NOT add DOPAMINE to any alkaline diluent solution,
since the drug is inactivated in alkaline solution.
IMPORTANT - Antidote for Peripheral Ischemia
- To prevent sloughing and necrosis in ischemic
areas, the area should be infiltrated as soon as
possible with 10 to 15 mL of saline solution
containing 5 to 10 mg of Regitine (brand of
phentolamine), an adrenergic blocking agent.
25
PRECAUTIONS:
Careful monitoring required
Hypoxia, Hypercapnia, Acidosis
Ventricular Arrhythmias
Decreased Pulse Pressure
Hypotension
Extravasation
Occlusive vascular disease
Weaning Labor and Delivery:
26
Nursing Mothers:
Paediatric Use: Peripheral gangrene has
been reported in neonates and children.
OVERDOSE
Since the duration of action of DOPAMINE
is quite short, no additional remedial
measures are usually necessary.
CONTRAINDICATIONS:
pheochromocytoma.
uncorrected tachyarrhythmia or
ventricular fibrillation.
27
CLINICAL PHARMACOLOGY
Dopamine is a natural catecholamine .
Dopamine produces positive chronotropic and
inotropic effects on the myocardium, resulting
in increased heart rate and cardiac contractility.
This is accomplished directly by exerting an
agonist action on beta-adrenoceptors and
indirectly by causing release of norepinephrine
from storage sites in sympathetic nerve
endings.
Dopamine's onset of action occurs within five
minutes of intravenous administration.
28
ADRENALINE:
Indications contd
as a hemostatic agent.
treating mucosal congestion of hay fever, rhinitis, and acute sinusitis;
to relieve bronchial asthmatic paroxysms;
in syncope due to complete heart block or carotid sinus
hypersensitivity;
for symptomatic relief of serum sickness, urticaria, angioneurotic
edema
for resuscitation in cardiac arrest following anesthetic accidents;
in simple (open angle) glaucoma;
for relaxation of uterine musculature and to inhibit uterine
contractions.
Epinephrine injection can be utilized to prolong the action of
intraspinal and local anesthetics
30
0.2 to 1 mL (mg). Start with a small dose and increase if required For
cardiac resuscitation.
STORAGE:
Store between 15 and 25C (59 and 77F),Protect from light and
freezing.
SIDE EFFECTS:
Transient and minor side effects of anxiety, headache, fear, and
palpitations often occur with therapeutic doses, especially in
hyperthyroid individuals. Repeated local injections can result in
necrosis at sites of injection from vascular constriction. Epinephrinefastness can occur with prolonged use
DRUG INTERACTIONS
Use of epinephrine with excessive doses of digitalis, diuretics, or other
drugs that sensitize the heart to arrhythmias is not recommended.
The effects of epinephrine may be potentiated by tricyclic
antidepressants; certain antihistamines, e.g., diphenhydramine
31
WARNINGS:
Administer with caution to elderly people; to those
with cardiovascular disease, hypertension, diabetes,
or hyperthyroidism; in psychoneurotic individuals;
and in pregnancy.
Overdosage or inadvertent intravenous injection of
epinephrine may cause cerebrovascular hemorrhage
resulting from the sharp rise in blood pressure.
PRECAUTIONS
Adrenalin (epinephrine injection,) should be
protected from exposure to light. The solution should
not be used if it is pinkish or darker than slightly
yellow or if it contains a precipitate.
Epinephrine is readily destroyed by alkalies and
oxidizing agents.
32
CONTRAINDICATIONS
narrow angle (congestive) glaucoma, shock, during
general anaesthesia with halogenated hydrocarbons or
cyclopropane and in individuals with organic brain
damage. local anesthesia of certain areas, e.g., fingers,
toes, because of the danger of vasoconstriction producing
sloughing of tissue; in labour because it may delay the
second stage; in cardiac dilatation and coronary
insufficiency.
CLINICAL PHARMACOLOGY
Adrenaline (epinephrine) is a sympathomimetic drug. It
activates an adrenergic receptive mechanism on effector
cells and imitates all actions of the sympathetic nervous
system except those on the arteries of the face and sweat
glands. Epinephrine acts on both alpha and beta receptors
and is the most potent alpha receptor activator.
33
DOBUTAMINE:
INDICATIONS
Depressed contractility resulting either from organic heart
disease or from cardiac surgical procedures.
Congestive heart failure.
DOSAGE AND ADMINISTRATION
NoteDo not add dobutamine to 5% Sodium Bicarbonate
Injection or to any other strongly alkaline solution.
Preparation and Stability At the time of administration,
dobutamine must be further diluted in an IV container to at
least a 50 mL solution using one of the following intravenous
solutions as a diluent: 5% Dextrose Injection, 5% Dextrose
and 0.45% Sodium Chloride Injection, 5% Dextrose and 0.9%
Sodium Chloride Injection, 10% Dextrose Injection, IsolyteM
with 5% Dextrose Injection, Lactated Ringer's Injection, 5%
Dextrose in Lactated Ringer's Injection.
34
SIDE EFFECTS
Increased Heart Rate, Blood Pressure, and Ventricular Ectopic Activity
Hypotension
Reactions at Sites of Intravenous Infusion Miscellaneous
Uncommon Effects
DRUG INTERACTIONS:
Preliminary studies indicate that the concomitant use of dobutamine
and nitroprusside results in a higher cardiac output and, usually, a
lower pulmonary wedge pressure than when either drug is used alone.
WARNINGS
Increase in Heart Rate or Blood Pressure
Ectopic Activity
Hypersensitivity
PRECAUTIONS
During the administration of dobutamine, as with any adrenergic
agent, ECG and blood pressure should be continuously monitored. In
addition, pulmonary wedge pressure and cardiac output should be
monitored .
Usage Following Acute Myocardial Infarction
35
OVERDOSE
Signs and Symptoms Toxicity from dobutamine is usually due
to excessive cardiac -receptor stimulation.
Treatment The initial actions to be taken in a dobutamine
overdose are discontinuing administration, establishing an airway,
and ensuring oxygenation and ventilation. Resuscitative measures.
CONTRAINDICATIONS
idiopathic hypertrophic subaortic stenosis and in patients who have
shown previous manifestations of hypersensitivity to dobutamine.
CLINICAL PHARMACOLOGY
Dobutamine is a direct-acting inotropic agent whose primary
activity results from stimulation of the receptors of the heart
while producing comparatively mild chronotropic, hypertensive,
arrhythmogenic, and vasodilative effects. It does not cause the
release of endogenous norepinephrine, as does dopamine
Systemic vascular resistance is usually decreased with
administration of dobutamine. Occasionally, minimum
vasoconstriction has been observed.
36
ESMOLOL
100 mg, 10 mL Single Dose Vial - Each mL contains 10 mg Esmolol
Hydrochloride, 5.9 mg Sodium Chloride,
100 mg, 5 mL DOUBLE STRENGTH Single Dose Vial - Each mL
contains 20 mg Esmolol Hydrochloride, 4.1 mg Sodium Chloride
INDICATIONS
Supraventricular Tachycardia,Intraoperative and Postoperative Tachycardia
and/or Hypertension
DOSAGE AND ADMINISTRATION
SUPRAVENTRICULAR TACHYCARDIA
An initial loading dose of 0.5 milligrams/kg (500 micrograms/kg) infused
over a minute duration followed by a maintenance infusion of 0.05
milligrams/kg/min (50 micrograms/kg/min) for the next 4 minutes is
recommended.
After the 4 minutes of initial maintenance infusion (total treatment
duration being 5 minutes), depending upon the desired ventricular
response, the maintenance infusion may be continued at 0.05 mg/kg/min
or increased step-wise (e.g. 0.1 mg/kg/min, 0.15 mg/kg/min to a maximum
of 0.2 mg/kg/min) with each step being maintained for 4 or more minutes.
37
SIDE EFFECTS
supraventricular tachycardia
hypotension
Cardiovascular -Symptomatic hypotension (diaphoresis,
dizziness)
Central Nervous System -Dizziness; somnolence ,confusion,
headache, and agitation and fatigue .Paresthesia, asthenia,
depression, abnormal thinking, anxiety, anorexia, and
lightheadedness were reported in less than 1% of patients.
Respiratory -Bronchospasm, wheezing, dyspnea, nasal
congestion, rhonchi, and rales have each been reported in
less than 1% of patients.
Gastrointestinal -Nausea. Vomiting, Dyspepsia,
constipation, dry mouth, and abdominal discomfort
Skin (Infusion Site)-Infusion site reactions including
inflammation and induration Edema, erythema, skin
discoloration, burning at the infusion site, thrombophlebitis,
39
and local skin necrosis from extravasation.
OVERDOSE
Acute Toxicity
Cardiac arrest.
Bradycardia, hypotension.
Bronchospasm
Cardiac Failure
CONTRAINDICATIONS
Sinus bradycardia, heart block greater than first
degree, cardiogenic shock or overt heart failure
CLINICAL PHARMACOLOGY
BREVIBLOC inhibits the beta1 receptors located
chiefly in cardiac muscle, but this preferential
effect is not absolute and at higher doses it begins
to inhibit beta2 receptors located chiefly in the
bronchial and vascular musculature.
40
KETAMINE
HYDROCHLORIDE:
INDICATIONS
DOSAGE:
As with other general anesthetic agents, the individual
response to ketamine is somewhat varied depending on
the dose, route of administration, and age of patient, so
that dosage recommendation cannot be absolutely
fixed. The drug should be titrated against the patient's
requirements.
42
HOW SUPPLIED
Each 10 mL vial contains 50 mg/mL, Protect from light.
SIDE EFFECTS
Cardiovascular- Blood pressure and pulse rate are
frequently elevated following administration of ketamine
alone.
Respiration -depression of respiration or apnea may occur
following rapid intravenous administration of high doses of
ketamine. Laryngospasms
Eye -Diplopia and nystagmus have been noted following
ketamine administration.
Neurological -In some patients, enhanced skeletal muscle
tone may be manifested by tonic and clonic movements
sometimes resembling seizures
Gastrointestinal -Anorexia, nausea and vomiting have been
observed; however, this is not usually severe and allows the
great majority of patients to take liquids by mouth shortly
after regaining consciousness
44
General -Anaphylaxis.
DRUG INTERACTIONS
Prolonged recovery time may occur if barbiturates
and/or narcotics are used concurrently with
ketamine.
PRECAUTIONS
Ketamine should be used by or under the
direction of physicians experienced in
administering general anesthetics and in
maintenance of an airway and in the control of
respiration.
Because pharyngeal and laryngeal reflexes are
usually active, ketamine should not be used alone
in surgery or diagnostic procedures of the
pharynx, larynx, or bronchial tree. Mechanical
stimulation of the pharynx should be avoided,
45
whenever possible, if ketamine is used alone.
OVERDOSE
Respiratory depression may occur
with over dosage or too rapid a rate
of administration of ketamine,
WARNINGS
Cardiac function ,hypertension or
cardiac decompensation.
Postoperative confusional states
Respiratory depression may occur
46
CONTRAINDICATIONS
elevation of blood pressure ,hypersensitivity
to the drug.
CLINICAL PHARMACOLOGY
Ketamine is a rapid-acting general
anesthetic producing an anesthetic state
characterized by profound analgesia,
normal pharyngeal-laryngeal reflexes,
normal or slightly enhanced skeletal muscle
tone, cardiovascular and respiratory
stimulation, and occasionally a transient
and minimal respiratory depression.
47
XYLOCAINE:
Xylocaine (lidocaine HCl) Injection, USP Xylocaine (lidocaine
HCl and epinephrine) Injection, For Infiltration and Nerve Block
DRUG DESCRIPTION
Xylocaine (lidocaine HCl) Injections are sterile, nonpyrogenic,
aqueous solutions that contain a local anesthetic agent with or
without epinephrine and are administered parenterally by injection.
INDICATIONS
local or regional anesthesia
DOSAGE AND ADMINISTRATION
The actual volumes and concentrations to be used depend on a
number of factors such as type and extent of surgical procedure,
depth of anesthesia and degree of muscular relaxation required,
duration of anesthesia required, and the physical condition of the
patient.
For intravenous regional anesthesia, only the 50 mL single dose vial
containing Xylocaine (lidocaine HCl) 0.5% Injection should be used.
48
Epidural Anesthesia
For epidural anesthesia, only the following dosage
forms Xylocaine Injection are recommended:
1% without epinephrine
1% with epinephrine
Caudal and Lumbar Epidural Block
As a precaution against the adverse experience
sometimes observed following unintentional
penetration of the subarachnoid space, a test
dose such as 2 to 3 mL of 1.5% lidocaine HCl
should be administered at least 5 minutes prior to
injecting the total volume required for a lumbar or
caudal epidural block. The test dose should be
repeated if the patient is moved in a manner that
may have displaced the catheter
49
SIDE EFFECTS
Central Nervous System -CNS manifestations are
excitatory and/or depressant and may be characterized by
lightheadedness, nervousness, apprehension, euphoria,
confusion, dizziness, drowsiness, tinnitus, blurred or double
vision, vomiting, sensations of heat, cold or numbness,
twitching, tremors, convulsions, unconsciousness,
respiratory depression and arrest.
Cardiovascular System -Cardiovascular manifestations
are usually depressant and are characterized by
bradycardia, hypotension, and cardiovascular collapse,
which may lead to cardiac arrest.
Allergic -Allergic reactions are characterized by cutaneous
lesions, urticaria, edema or anaphylactoid reactions.
Neurologic-positional headaches, hypotension and
backache; 2 percent for shivering; and less than 1 percent
each for peripheral nerve symptoms, nausea, respiratory
inadequacy and double vision. Many of these observations
50
may be related to local anesthetic techniques, with or
DRUG INTERACTIONS
Clinically Significant Drug Interactions
The administration of local anesthetic solutions
containing epinephrine or norepinephrine to
patients receiving monoamine oxidase inhibitors
or tricyclic antidepressants may produce severe,
prolonged hypertension.
Phenothiazines and butyrophenones may reduce
or reverse the pressor effect of epinephrine.
Drug/Laboratory Test Interactions
The intramuscular injection of lidocaine HCl may
result in an increase in creatine
phosphokinase levels.
51
WARNINGS
immediate availability of oxygen, other
resuscitative drugs, cardiopulmonary
equipment and the personnel needed for
proper management of toxic reactions and
related emergencies. delay in proper
management of dose-related toxicity,
underventilation from any cause and/or altered
sensitivity may lead to the development of
acidosis, cardiac arrest and, possibly, death.
PRECAUTIONS
Resuscitative equipment, oxygen, and other
resuscitative drugs should be available for immediate
use
52
CONTRAINDICATIONS
known history of hypersensitivity to local anesthetics of
the amide type.
CLINICAL PHARMACOLOGY
Mechanism of Action
Lidocaine HCl stabilizes the neuronal membrane by
inhibiting the ionic fluxes required for the initiation and
conduction of impulses thereby effecting local anesthetic
action.
PRIMACOR IV
PRIMACOR (milrinone lactate 5% Dextrose
Injection
INDICATIONS
patients with acute decompensated heart failure
53
54
SIDE EFFECTS
Cardiovascular Effects: ventricular arrhythmias ,Ventricular
ectopic activity, nonsustained ventricular tachycardia, sustained
ventricular tachycardia, 1% and ventricular fibrillation, Other
cardiovascular adverse reactions include hypotension, 2.9% and
angina/chest pain, 1.2%.
CNS Effects -Headaches, usually mild to moderate in severity,
have been reported in 2.9% of patients receiving PRIMACOR.
Other Effects -Other adverse reactions reported, but not
definitely related to the administration of PRIMACOR include
hypokalemia, 0.6%; tremor, 0.4%; and thrombocytopenia, 0.4%.
Post-Marketing Adverse Event Reports
Isolated spontaneous reports of bronchospasm and anaphylactic
shock.
Liver function test abnormalities and skin reactions such as
rash.
Administration site conditions: Infusion site reaction.
55
PRECAUTIONS
severe obstructive aortic or pulmonic valvular disease
Supraventricular and ventricular arrhythmias
If prior vigorous diuretic therapy is suspected to have
caused significant decreases in cardiac filling pressure,
OVERDOSE
produce hypotension because of its vasodilator effect.
If this occurs, administration of PRIMACOR should be
reduced or temporarily discontinued until the patient's
condition stabilizes. No specific antidote is known.
CONTRAINDICATIONS
PRIMACOR is contraindicated in patients who are
hypersensitive to it.
56
CLINICAL PHARMACOLOGY
PRIMACOR is a positive inotrope and vasodilator,
with little chronotropic activity different in
structure and mode of action from either the
digitalis glycosides or catecholamines.
PRIMACOR, at relevant inotropic and vasorelaxant
concentrations, is a selective inhibitor of peak III
cAMP phosphodiesterase isozyme in cardiac and
vascular muscle. This inhibitory action is
consistent with cAMP mediated increases in
intracellular ionized calcium and contractile force
in cardiac muscle, as well as with cAMP
dependent contractile protein phosphorylation
and relaxation in vascular muscle.
57
NALAXONE
NARCAN (naloxone hydrochloride) Injection, Opioid Antagonist
INDICATIONS
complete or partial reversal of opioid depression, including
respiratory depression,
diagnosis of suspected or known acute opioid over dosage.
NARCAN may be useful as an adjunctive agent to increase blood
pressure in the management of septic shock.
DOSAGE AND ADMINISTRATION:
NARCAN may be administered intravenously, intramuscularly, or
subcutaneously.
NARCAN may be diluted for intravenous infusion in normal saline
or 5% dextrose solutions. The addition of 2 mg of NARCAN in 500
mL of either solution provides a concentration of 0.004 mg/mL.
Mixtures should be used within 24 hours. After 24 hours, the
remaining unused mixture must be discarded. The rate of
administration should be titrated in accordance with the patient's
response.
58
DRUG INTERACTIONS
Large doses of naloxone are required to antagonize
buprenorphine since the latter has a long duration of action
due to its slow rate of binding and subsequent slow
dissociation from the opioid receptor.
WARNINGS
Drug Dependence
Respiratory Depression due to Other Drugs
Renal Insufficiency/Failure
The safety and effectiveness of NARCAN in patients with
renal insufficiency/failure have not been established in wellcontrolled clinical trials
Liver Disease
liver disease
CONTRAINDICATIONS
hypersensitive to naloxone hydrochloride
60
CLINICAL PHARMACOLOGY
Complete or Partial Reversal of Opioid
While the mechanism of action of NARCAN is not
fully understood, in vitro evidence suggests that
NARCAN antagonizes opioid effects by competing
for the , and opiate receptor sites in the
CNS, with the greatest affinity for the receptor.
Adjunctive Use in Septic Shock
NARCAN has been shown in some cases of septic
shock to produce a rise in blood pressure that
may last up to several hours; however, this
pressor response has not been demonstrated to
improve patient survival
61
NICARDIPINE:
Cardene (nicardipine hydrochloride) is a calcium ion influx
inhibitor (slow channel blocker or calcium channel blocker).
Cardene I.V. Premixed Injection for intravenous administration
contains 20 mg of nicardipine hydrochloride per 200 mL (0.1
mg/mL) in either dextrose or sodium chloride.
INDICATIONS
Hypertension
DOSAGE AND ADMINISTRATION
Recommended Dosing
Cardene I.V. is intended for intravenous use. Titrate dose to
achieve the desired blood pressure reduction. Individualize
dosage depending on the blood pressure to be obtained and
the response of the patient.
Dosage as a Substitute for Oral Nicardipine Therapy
The intravenous infusion rate required to produce an average
plasma concentration equivalent to a given oral dose
62
HOW SUPPLIED
Dosage Forms And Strengths
Cardene I.V. Premixed Injection is supplied as a single-use, ready-to-use, isoosmotic solution for intravenous administration in a 200 mL GALAXY container
with 20 mg (0.1 mg/mL) nicardipine hydrochloride in either dextrose or
sodium chloride.
SIDE EFFECTS
Adverse Reactions Observed in Clinical Trials
Body as a Whole: fever, neck pain Cardiovascular: angina pectoris,
atrioventricular block, ST segment depression, inverted T wave, deep-vein
thrombophlebitis
Digestive: dyspepsia
Hemic and Lymphatic: thrombocytopenia
Metabolic and Nutritional: hypophosphatemia, peripheral edema
Nervous: confusion, hypertonia
Respiratory: respiratory disorder
Special Senses: conjunctivitis, ear disorder, tinnitus
Urogenital: urinary frequency
DRUG INTERACTIONS
Beta-Blockers, Cimetidine, Cyclosporine
63
PRECAUTIONS
Excessive Pharmacodynamic Effects
Use in Patients with Angina
Use in Patients with Heart Failure
Use in Patients with Impaired Hepatic Function
Use in Patients with Impaired Renal Function
Intravenous Infusion Site
CONTRAINDICATIONS -Advanced Aortic Stenosis
Mechanism of Action
Nicardipine inhibits the transmembrane influx of
calcium ions into cardiac muscle and smooth
muscle without changing serum calcium
concentrations.
64
NITROSTAT DRUG
HOW SUPPLIED
Nitrostat is supplied as white, round, flat-faced
tablets in 3 strengths (0.3 mg, 0.4 mg, and 0.6 mg)
in bottles containing 100 tablets each, with colorcoded labels, and in color-coded Patient
0.3 mg, 0.4 mg, 0.6 mg
Store at Controlled Room Temperature 20-25C
(68-77F)
SIDE EFFECTS
Headache which may be severe and persistent
may occur immediately after use. Vertigo,
dizziness, weakness, palpitation, and other
manifestations of postural hypotension may
develop occasionally, particularly in erect,
immobile patients.
66
DRUG INTERACTIONS
Patients receiving antihypertensive drugs, beta-adrenergic
blockers, or phenothiazines and nitrates should be
observed for possible additive hypotensive effects.
The vasodilatory and hemodynamic effects of
nitroglycerin maybe enhanced by concomitant
administration of aspirin
Tricyclic antidepressants (amitriptyline, desipramine,
doxepin, others) and anticholinergic drugs may cause dry
mouth and diminished salivary secretions.
patients receiving sublingual nitroglycerin should avoid
ergotamine and related drugs or be monitored for
symptoms of ergotism if this is not possible
Drug/Laboratory Test Interactions
false report of decreased serum cholesterol.
67
PRECAUTIONS:
General
Only the smallest dose required for effective relief of the acute
anginal attack should be used. Excessive use may lead to the
development of tolerance.
OVERDOSE:
Hemodynamic Effects
The effects of nitroglycerin overdose are generally the results of
nitroglycerin's capacity to induce vasodi-latation, venous pooling,
reduced cardiac output, and hypotension. including increased
intracranial pressure, with any or all of persistent throbbing
headache, confusion, and moderate fever; vertigo; palpitations;
tachycardia; visual disturbances; nausea and vomiting (possibly
with colic and even bloody diarrhea); syncope (especially in the
upright posture); dyspnea, later followed by reduced ventilatory
effort, diaphoresis, with the skin either flushed or cold and clammy;
heartblock and bradycardia; paralysis; coma; seizures; and death.
Methemoglobinemia -rarely reported
68
CONTRAINDICATIONS
early myocardial infarction, severe anemia, increased
intracranial pressure, and those with a known
hypersensitivity to nitroglycerin.
CLINICAL PHARMACOLOGY
The principal pharmacological action of nitroglycerin is
relaxation of vascular smooth muscle. Although
venous effects predominate, nitroglycerin produces, in a
dose-related manner, dilation of both arterial and
venous beds. Dilation of postcapillary vessels, including
large veins, promotes peripheral pooling of blood,
decreases venous return to the heart, and reduces left
ventricular end-diastolic pressure (preload). Nitroglycerin
also produces arteriolar relaxation, thereby reducing
peripheral vascular resistance and arterial pressure
(afterload), and dilates large epicardial coronary arteries;69
NITROPRESS
WARNINGS
The principal hazards of NITROPRESS administration
are excessive hypotension and excessive accumulation
of cyanide
Excessive Hypotension
PRECAUTIONS
General -Like other vasodilators, sodium nitroprusside
can cause increases in intracranial pressure..
Hepatic -Use caution when administering nitroprusside
to patients with hepatic insufficiency.
Use in Anesthesia -When sodium nitroprusside (or
any other vasodilator) is used for controlled
hypotension during anesthesia, the patient's capacity
to compensate for anemia and hypovolemia may be
diminished.
72
OVERDOSE
Overdosage of nitroprusside can be manifested
as excessive hypotension or cyanide toxicity .
Treatment of cyanide toxicity:
Treatment of cyanide toxicity consists of
discontinuing the administration of sodium
nitroprusside;
providing a buffer for cyanide by using sodium
nitrite to convert as much haemoglobin into
methemoglobin as the patient can safely
tolerate; and then
infusing sodium thiosulfate in sufficient
quantity to convert the cyanide into thiocyanate.
73
CONTRAINDICATIONS
treatment of compensatory hypertension,to
produce hypotension during surgery in
patients with known inadequate cerebral
circulation, for the treatment of acute
congestive heart failure
CLINICAL PHARMACOLOGY
The principal pharmacological action of
sodium nitroprusside is relaxation of vascular
smooth muscle and consequent dilatation of
peripheral arteries and veins. Other smooth
muscle (e.g. , uterus, duodenum) is not
affected.
74
NOREPINEPHRINE:
Norepinephrine is a sympathomimetic amine which differs from
epinephrine by the absence of a methyl group on the nitrogen atom
INDICATIONS
For blood pressure control in certain acute hypotensive states
As an adjunct in the treatment of cardiac arrest and profound
hypotension.
DOSAGE AND ADMINISTRATION
Diluent: LEVOPHED should be diluted in 5 percent dextrose injection or
5 percent dextrose and sodium chloride injections. These dextrose
containing fluids are protection against significant loss of potency due
to oxidation. Administration in saline solution alone is not
recommended. Whole blood or plasma, if indicated to increase blood
volume, should be administered separately (for example, by use of a Ytube and individual containers if given simultaneously).
Average Dosage: Add the content of the vial (4 mg/4 mL) of
LEVOPHED to 1,000 mL of a 5 percent dextrose containing solution.
Duration of Therapy: The infusion should be continued until adequate
blood pressure and tissue perfusion are maintained without therapy.
75
DRUG INTERACTIONS
Cyclopropane and halothane anesthetics
increase cardiac autonomic irritability and
therefore seem to sensitize the myocardium
to the action of intravenously administered
epinephrine or norepinephrine.
DRUG INTERACTIONS
Cyclopropane and halothane anesthetics
increase cardiac autonomic irritability and
therefore seem to sensitize the myocardium
to the action of intravenously administered
epinephrine or norepinephrine.
77
OVERDOSE
Overdosage with LEVOPHED may result in headache, severe
hypertension, reflex bradycardia, marked increase in
peripheral resistance, and decreased cardiac output. In case
of accidental overdosage, as evidenced by excessive blood
pressure elevation, discontinue LEVOPHED until the
condition of the patient stabilizes.
CONTRAINDICATIONS
LEVOPHED should not be given to patients who are
hypotensive from blood volume deficits except as an
emergency measure to maintain coronary and cerebral
artery perfusion until blood volume replacement therapy can
be completed.
CLINICAL PHARMACOLOGY
LEVOPHED functions as a peripheral vasoconstrictor (alphaadrenergic action) and as an inotropic stimulator of the heart
and dilator of coronary arteries (beta-adrenergic action).
78
PENTOBARBITOL:
79
HOW SUPPLIED
NEMBUTAL Sodium Solution (pentobarbital sodium injection,
USP) is available in the following sizes:
20-mL multiple-dose vial, 1 g per vial and 50-mL multipledose vial, 2.5 g per vial
Each mL contains:
Pentobarbital Sodium, derivative of barbituric
acid.......................................50 mg
Propylene
glycol.....................................................................................
...40% v/v
Alcohol ..................................................................................
..........................10%
Water for
Injection.................................................................................
.............qs (pH adjusted to approximately 9.5 with
hydrochloric acid and/or sodium hydroxide.)
81
DRUG INTERACTIONS
Anticoagulants
Corticosteroids:
Doxycycline:
Phenytoin, sodium valproate, valproic acid:
Central nervous system depressants:
Monoamine oxidase inhibitors (MAOI):
Estradiol, estrone, progesterone and other steroidal hormones:
Habit forming:
Acute or chronic pain:
PRECAUTIONS
Barbiturates may be habit forming.
In patients with hepatic damage, barbiturates should be
administered with caution and initially in reduced doses.
Barbiturates should not be administered to patients showing
the premonitory signs of hepatic coma.
83
PRECAUTIONS
Barbiturates may be habit forming.
In patients with hepatic damage
signs of hepatic coma.
OVERDOSE
The toxic dose of barbiturates varies considerably. In
general, an oral dose of 1 gram of most barbiturates
produces serious poisoning in an adult. Death
commonly occurs after 2 to 10 grams of ingested
barbiturate. CONTRAINDICATIONS
Barbiturates are contraindicated in patients with
known barbiturate sensitivity. Barbiturates are also
contraindicated in patients with a history of manifest
or latent porphyria.
84
CLINICAL PHARMACOLOGY
Barbiturates are capable of producing all
levels of CNS mood alteration from excitation
to mild sedation, to hypnosis, and deep coma.
Overdosage can produce death. In high
enough therapeutic doses, barbiturates
induce anesthesia.
Barbiturates depress the sensory cortex,
decrease motor activity, alter cerebellar
function, and produce drowsiness, sedation,
and hypnosis.
Barbiturate-induced sleep differs from
physiological sleep.
85
SIDE EFFECTS
The most common adverse reactions to oral potassium salts are
nausea, vomiting, flatulence, abdominal pain/discomfort, and
diarrhea.
DRUG INTERACTIONS-Potassium-sparing diuretics, angiotensin
converting enzyme inhibitors .
Hyperkalemia
In patients with impaired mechanisms for excreting potassium, the
administration of potassium salts can produce hyperkalemia and
cardiac arrest.
Hypokalemia should not be treated by the concomitant
administration of potassium salts and a potassium-sparing diuretic,
e.g., spironolactone
Angiotensin converting enzyme (ACE) inhibitors (e.g., captopril,
enalapril) will produce some potassium retention by inhibiting
aldosterone production.
87
LABORATORY TESTS
OVERDOSE
The administration of oral potassium salts
to persons with normal excretory
mechanisms for potassium rarely causes
serious hyperkalemia.
Intravenous administration of 300 to 500
ml/hr of 10% dextrose solution containing
10-20 units of crystalline insulin per 1,000
ml;
Correction of acidosis, if present, with
intravenous sodium bicarbonate;
88
CONTRAINDICATIONS
chronic renal failure, systemic acidosis such as
diabetic acidosis, acute dehydration, extensive
tissue breakdown as in severe burns, adrenal
insufficiency, or the administration of a potassiumsparing diuretic.
CLINICAL PHARMACOLOGY
Potassium ion is the principal intracellular cation of
most body tissues. Potassium ions participate in a
number of essential physiological processes
including the maintenance of intracellular tonicity,
the transmission of nerve impulses, the contraction
of cardiac, skeletal and smooth muscle, and the
maintenance of normal renal function.
89
PROCAINAMIDE:
INDICATIONS
ventricular arrhythmias, ventricular tachycardia.
DOSAGE AND ADMINISTRATION
To provide approximately 50 mg per kg of body weight per day*
SIDE EFFECTS
Cardiovascular
Hypotension and serious disturbances of cardiorhythm such as
ventricular asystole or fibrillation are more common after
Second degree heart block has been reported in 2 of almost 500
patients taking PA orally.
Multisystem
A lupus erythematosus-like syndrome of arthralgia, pleural or
abdominal pain,
Hematologic
Neutropenia, thrombocytopenia, or hemolytic anaemia
90
Skin
Angioneurotic oedema, urticaria, pruritus, flushing, and
maculopapular rash have also occurred occasionally.
Gastrointestinal
Anorexia, nausea, vomiting, abdominal pain, bitter taste, or diarrhea
Elevated Liver Enzymes
Elevations of transaminase with and without elevations of alkaline
phosphatase and bilirubin have been reported.
Nervous System
Dizziness or giddiness, weakness, mental depression, and psychosis
with hallucinations
DRUG INTERACTIONS
If other antiarrhythmic drugs are being used, additive effects on the
heart may occur with PA administration, and dosage reduction may
be necessary.
Anticholinergic drugs administered concurrently with PA may produce
additive antivagal effects on A-V nodal conduction, although this is
not as well documented for PA as for quinidine.
91
Patients weighing
lb
kg
88-110
40-50
250mgq3hto500mgq6h
132-154
60-70
375mgq3hto750mgq6h
176-198
80-90
500mgq3hrto1gq6h
>220
>100
625mgq3hto1.25gq6h
WARNINGS
Blood Dyscrasias
Digitalis Intoxication
First Degree Heart Block
Predigitalization for Atrial Flutter or Fibrillation
Patients with atrial flutter or fibrillation
Congestive Heart Failure
Concurrent Other Antiarrhythmic Agents
Renal insufficiency
Myasthenia Gravis
93
PRECAUTIONS:
Immediately after initiation of PA therapy, patients
should be closely observed for possible
hypersensitivity reactions, especially if procaine
or local anaesthetic sensitivity is suspected, and
for muscular weakness if myasthenia gravis is a
possibility.
Laboratory Tests
Laboratory tests such as complete blood count
(CBC), electrocardiogram, and serum creatinine or
urea nitrogen may be indicated, depending on the
clinical situation, and periodic rechecking of the
CBC and ANA may be helpful in early detection of
untoward reactions.
94
CONTRAINDICATIONS
Complete Heart Block
Idiosyncratic Hypersensitivity
Lupus Erythematosus
Torsades de Pointes
CLINICAL PHARMACOLOGY
Procainamide (PA) increases the effective refractory
period of the atria, and to a lesser extent the bundle of
His-Purkinje system and ventricles of the heart. It
reduces impulse conduction velocity in the atria, HisPurkinje fibers, and ventricular muscle, but has
variable effects on the atrioventricular (A-V) node, a
direct slowing action and a weaker vagolytic effect
which may speed A-V conduction slightly. Myocardial
excitability is reduced in the atria.
95
DIPRIVAN
(PROPOFOL) INJECTABLE EMULSION
FOR IV ADMINISTRATION:
INDICATIONS
DIPRIVAN Injectable Emulsion is an IV sedative-hypnotic agent that can be used
as described in the table below.
Table 3. Indications for DIPRIVAN Injectable Emulsion
Indication
Approved Patient Population
Initiation and maintenance of Monitored Anesthesia Care (MAC) sedation
Adults only
Combined sedation and regional anesthesia
Adults only
Induction of General Anesthesia
Patients 3 years of age
Mainenance of General Anesthesia
Patients 2 months of age
Intensive Care Unit (ICU) sedation of intubated, mechanically ventilated patients
Adults only
DIPRIVAN Injectable Emulsion is not indicated for use in Pediatric ICU sedation
since the safety of this regimen has not been established
96
HANDLING PROCEDURES
Parenteral drug products should be inspected visually for particulate
matter and discoloration prior to administration whenever solution
and container permit.
Do not use if there is evidence of separation of the phases of the
emulsion.
There have been reports in which failure to use aseptic technique
when handling Diprivan Injectable Emulsion was associated with
microbial contamination of the product and with fever,
infection/sepsis, other life-threatening illness, and/or death.
Diprivan, with EDTA, inhibits microbial growth for up to 12 hours, as
demonstrated by test data for representative USP microorganisms.
HOW SUPPLIED
DIPRIVAN Injectable Emulsion is available as follows:
Propofol undergoes oxidative degradation, in the presence of oxygen,
and is therefore packaged under nitrogen to eliminate this
degradation path.
Store between 4-22C (40-72F). Do not freeze. Shake well before
use.
98
DRUG INTERACTIONS
The induction dose requirements of DIPRIVAN Injectable
Emulsion may be reduced in patients with intramuscular or
intravenous premedication, particularly with narcotics (e.g.,
morphine, meperidine, and fentanyl, etc.) and combinations
of opioids and sedatives.
WARNINGS
Use of DIPRIVAN Injectable Emulsion has been associated
with both fatal and life- threatening anaphylactic and
anaphylactoid reactions.
Sedated patients should be continuously monitored, and
facilities for maintenance of a patent airway, providing
artificial ventilation, administering supplemental oxygen, and
instituting cardiovascular resuscitation must be immediately
available. Patients should be continuously monitored for
early signs of hypotension, apnea, airway obstruction, and/or
oxygen desaturation.
99
OVERDOSE
If overdosage occurs, DIPRIVAN Injectable Emulsion administration should
be discontinued immediately. Overdosage is likely to cause
cardiorespiratory depression. Respiratory depression should be treated by
artificial ventilation with oxygen. Cardiovascular depression may require
repositioning of the patient by raising the patient's legs, increasing the
flow rate of intravenous fluids, and administering pressor agents and/or
anticholinergic agents.
PRECAUTIONS
General
Adult and Pediatric Patients: A lower induction dose and a slower
maintenance rate of administration should be used in elderly, debilitated,
patients. Patients should be continuously monitored for early signs of
hypotension and/or bradycardia. Apnea requiring ventilatory support often
occurs during induction and may persist for more than 60 seconds. Very
rarely the use of DIPRIVAN Injectable Emulsion may be associated with the
development of a period of postoperative unconsciousness which may be
accompanied by an increase in muscle tone. This may or may not be
preceded by a brief period of wakefulness.
Recovery is spontaneous.
100
CONTRAINDICATIONS
Hypersensitivity
Allergies to eggs, egg products, soybeans or soy
products
CLINICAL PHARMACOLOGY
DIPRIVAN Injectable Emulsion is an intravenous
sedative-hypnotic agent for use in the induction and
maintenance of anaesthesia or sedation. Intravenous
injection of a therapeutic dose of propofol induces
hypnosis, with minimal excitation, usually within 40
seconds from the start of injection (the time for one
arm-brain circulation). As with other rapidly acting
intravenous anaesthetic agents, the half-time of the
blood-brain equilibration is approximately 1 to 3
minutes, accounting for the rate of induction of
anaesthesia.
101
SIDE EFFECTS
Alkalosis
Hyperirritability or tetany
Febrile response,
Infection at the site of injection,
Venous thrombosis or phlebitis
extending from the site of injection,
Extravasation, and hypervolemia.
nate, USP in Water for Injection, USP.
103
WARNINGS
Rapid administration of sodium salts may precipitate volume
overload and acute pulmonary edema. Rapid or excessive
administration of Sodium Bicarbonate Injection may produce
tetany due to a decrease in ionized calcium and
hypokalemia as potassium reenters the cells.
Sodium containing solutions should be used with great care,
if at all, in patients with congestive heart failure, severe
renal insufficiency and in clinical states in which there exists
edema with sodium retention.
Excessive or too rapid administration of Sodium Bicarbonate
Injection may produce alkalosis.
PRECAUTIONS
Correction of acidosis without correction of a potassium
deficit may lead to severe hypokalemia. Coexistent
hypocalcemia may be associated with carpopedal spasm as
the plasma pH rises.
104
CONTRAINDICATIONS
Sodium Bicarbonate Injection is contraindicated in patients
with metabolic and respiratory alkalosis and in patients
with hypocalcemia in which alkalosis may produce tetany.
CLINICAL PHARMACOLOGY
The bicarbonate-carbonic acid system constitutes the
principal extracellular buffer. Increasing the bicarbonate
concentration buffers excess hydrogen ion concentration,
raises blood pH and reverses the clinical manifestations of
acidosis.
HOW SUPPLIED
Exposure of pharmaceutical products to heat should be
minimized. Avoid excessive heat. Protect from freezing. It is
recommended the product be stored at room temperature
(25C): brief exposure up to 40C does not adversely affect
the product.
105
VECURONIUM BROMIDE:
ZEMURON (rocuronium bromide) injection is a
nondepolarizing neuromuscular blocking agent
INDICATIONS
adjunct to general anaesthesia to facilitate both rapid
sequence and routine tracheal intubation, and to provide
skeletal muscle relaxation during surgery or mechanical
ventilation.
DOSAGE AND ADMINISTRATION
The recommended initial dose of ZEMURON, regardless of
anesthetic technique, is 0.6 mg/kg.
HOW SUPPLIED
ZEMURON (rocuronium bromide) injection is available as
5 mL multiple dose vials containing 50 mg rocuronium
bromide injection (10 mg/mL)
10 mL multiple dose vials containing 100 mg rocuronium
bromide injection (10 mg/mL)
106
SIDE EFFECTS
In clinical trials, the most common adverse reactions (2%)
are transient hypotension and hypertension.
The following adverse reactions are described, or
described in greater detail, in other sections:
Anaphylaxis
Residual paralysis
Myopathy
Increased pulmonary vascular resistance
Cardiovascular: arrhythmia, abnormal
electrocardiogram, tachycardia
Digestive: nausea, vomiting
Respiratory: asthma (bronchospasm, wheezing, or
rhonchi), hiccup
Skin and Appendages: rash, injection site edema,
pruritus
107
DRUG INTERACTIONS
Antibiotics
Drugs which may enhance the neuromuscular blocking action
of nondepolarizing agents such as ZEMURON include certain
antibiotics (e.g., aminoglycosides; vancomycin; tetracyclines;
bacitracin; polymyxins; colistin; and sodium colistimethate). If
these antibiotics are used in conjunction with ZEMURON,
prolongation of neuromuscular block may occur.
Anticonvulsants
In 2 of 4 patients receiving chronic anticonvulsant therapy,
apparent resistance to the effects of ZEMURON was observed
in the form of diminished magnitude of neuromuscular block,
or shortened clinical duration.
Lithium Carbonate
Lithium has been shown to increase the duration of
neuromuscular block and decrease infusion requirements of
neuromuscular blocking agents
108
SUCCINYLCHOLINE:
If ZEMURON is administered following administration of
succinylcholine, it should not be given until recovery from
succinylcholine has been observed.
PRECAUTIONS
The drug should not be administered unless facilities for
intubation, mechanical ventilation, oxygen therapy, and
an antagonist are immediately available. It is
recommended that clinicians administering
neuromuscular blocking agents such as ZEMURON employ
a peripheral nerve stimulator to monitor drug effect, need
for additional doses, adequacy of spontaneous recovery or
antagonism, and to decrease the complications of
overdosage if additional doses are administered.
Anaphylaxis
Extravasation
109
OVERDOSE
Overdosage with neuromuscular blocking agents may result in
neuromuscular block beyond the time needed for surgery and
anesthesia. The primary treatment is maintenance of a patent
airway, controlled ventilation and adequate sedation until recovery
of normal neuromuscular function is assured. Once evidence of
recovery from neuromuscular block is observed, further recovery
may be facilitated by administration of an anticholinesterase agent
in conjunction with an appropriate anticholinergic agent.
CONTRAINDICATIONS
hypersensitivity
CLINICAL PHARMACOLOGY
ZEMURON is a nondepolarizing neuromuscular blocking agent with
a rapid to intermediate onset depending on dose and intermediate
duration. It acts by competing for cholinergic receptors at the motor
end-plate. This action is antagonized by acetylcholinesterase
inhibitors, such as neostigmine and edrophonium.
110
THIOPENTAL: -PENTOTHAL
(thiopental sodium) for Injection
DRUG DESCRIPTION
The drug is prepared as a sterile powder and
after reconstitution with an appropriate diluent
is administered by the intravenous route.
The following diluents in various container,
syringe and vial sizes are provided in Pentothal
Kits, Pentothal Ready-to-Mix Syringes and Vials
for preparing solutions of Pentothal (Thiopental
Sodium for Injection, USP) for clinical use.
111
INDICATIONS
(1) as the sole anaesthetic agent for brief (15 minute)
procedures, (2) for induction of anesthesia prior to
administration of other anesthetic agents, (3) to
supplement regional anesthesia, (4) to provide hypnosis
during balanced anesthesia with other agents for
analgesia or muscle relaxation, (5) for the control of
convulsive states during or following inhalation
anesthesia, local anesthesia, or other causes, (6) in
neurosurgical patients with increased intracranial
pressure, if adequate ventilation is provided, and (7) for
narcoanalysis and narcosynthesis in psychiatric disorders.
DOSAGE AND ADMINISTRATION
Pentothal is administered by the intravenous route only
Premedication
Premedication usually consists of atropine or scopolamine
to suppress vagal reflexes and inhibit secretions.
112
Test Dose
It is advisable to inject a small "test" dose
of 25 to 75 mg (1 to 3 mL of a 2.5%
solution) of Pentothal to assess tolerance
or unusual sensitivity to Pentothal,
COMPLICATIONS
Respiratory depression
Laryngospasm
Myocardial depression,
Extra vascular infiltration
Shivering
113
DRUG INTERACTIONS
The following drug interactions have
been reported with thiopental.
Drug
Effect
Probenecid
Prolongedactionofthiopental
Diazoxide
Hypotension
Zimelidine
Thiopentalantagonism
Decreased
antinociceptive
Opioidanalgesics
Aminophylline
action
Thiopentalantagonism
Midazolam
Synergism
115
WARNINGS
Pentothal
KEEP RESUSCITATIVE AND
ENDOTRACHEAL INTUBATION EQUIPMENT
AND OXYGEN READILY AVAILABLE.
MAINTAIN PATENCY OF THE AIRWAY AT ALL
TIMES.
This drug should be administered only by
persons qualified in the use of intravenous
anesthetics.
Avoid extravasation or intra-arterial
injection.
116
PRECAUTIONS
Observe aseptic precautions
Care should be taken in administering the drug to patients
with advanced cardiac disease, increased intracranial
pressure, ophthalmoplegia plus, asthma, myasthenia gravis
and endocrine insufficiency (pituitary, thyroid, adrenal,
pancreas).
PentothalOverdosage:
may occur from too rapid or repeated injections. Too rapid
injection may be followed by an alarming fall in blood
pressure even to shock levels. Apnea, occasional
laryngospasm, coughing and other respiratory difficulties
with excessive or too rapid injections may occur. In the
event of suspected or apparent overdosage, the drug
should be discontinued, a patent airway established
(intubate if necessary) or maintained, and oxygen should be
administered, with assisted ventilation if necessary.
117
MANAGEMENT OF 0VERDOSAGE
CLINICAL PHARMACOLOGY
Pentothal (Thiopental Sodium for Injection, USP) is
an ultrashort-acting depressant of the central
nervous system which induces hypnosis and
anesthesia, but not analgesia. It produces hypnosis
within 30 to 40 seconds of intravenous injection.
Recovery after a small dose is rapid, with some
somnolence and retrograde amnesia. Repeated
intravenous doses lead to prolonged anesthesia
because fatty tissues act as a reservoir; they
accumulate Pentothal in concentrations 6 to 12
times greater than the plasma concentration, and
then release the drug slowly to cause prolonged
anesthesia.
119
PHENYTOIN:
DILANTIN
(PHENYTOIN SODIUM) 100 MG EXTENDED ORAL CAPSULE
Phenytoin sodium is an antiepileptic drug.
INDICATIONS
Dilantin is indicated for the control of generalized tonicclonic (grand mal) and complex partial (psychomotor,
temporal lobe) seizures and prevention and treatment of
seizures occurring during or following neurosurgery.
DOSAGE AND ADMINISTRATION
Dosage should be individualized to provide maximum
benefit. In some cases, serum blood level determinations
may be necessary for optimal dosage adjustmentsthe
clinically effective serum level is usually 10-20 mcg/mL.
120
Adult Dosage
Patients who have received no previous treatment may
be started on one 100-mg Dilantin (Phenytoin sodium)
Extended Oral Capsule three times daily and the
dosage then adjusted to suit individual requirements.
SIDE EFFECTS
Central Nervous System: nystagmus, ataxia, slurred
speech, decreased coordination, and mental confusion.
Dizziness, insomnia,
Gastrointestinal System: Nausea, vomiting,
constipation, toxic hepatitis, and liver damage.
Integumentary System: Dermatological
manifestations sometimes accompanied by fever have
included scarlatiniform or morbilliform rashes. A
morbilliform rash (measles-like) is the most common;
121
DRUG INTERACTIONS
Drugs which may increase phenytoin serum levels include:
acute alcohol intake, amiodarone, chloramphenicol,
chlordiazepoxide, cimetidine, diazepam, dicumarol, disulfiram,
estrogens, ethosuximide, fluoxetine, H2-antagonists,
halothane, isoniazid, methylphenidate, phenothiazines,
phenylbutazone, salicylates, succinimides, sulfonamides,
ticlopidine, tolbutamide, trazodone.
Drugs which may decrease phenytoin levels include:
carbamazepine, chronic alcohol abuse, reserpine, and
sucralfate. Moban brand of molindone hydrochloride contains
calcium ions which interfere with the absorption of phenytoin.
Ingestion times of phenytoin and antacid preparations
containing calcium should be staggered in patients with low
serum phenytoin levels to prevent absorption problems.
Phenytoin may decrease serum concentrations of T4
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WARNINGS
Abrupt withdrawal of phenytoin in epileptic patients may
precipitate status epilepticus.
PRECAUTIONS
The liver is the chief site of biotransformation of phenytoin;
patients with impaired liver function, elderly patients, or those
who are gravely ill may show early signs of toxicity.
A small percentage of individuals who have been treated with
phenytoin have been shown to metabolize the drug slowly.
Slow metabolism may be due to limited enzyme availability
and lack of induction; it appears to be genetically determined.
Phenytoin should be discontinued if a skin rash appears
Laboratory Tests
Phenytoin serum level determinations may be necessary to
achieve optimal dosage adjustments.
Treatment
Treatment is nonspecific since there is no known antidote.
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HYDROCORTISONE:
CORTEF (HYDROCORTISONE) TABLET
CORTEF Tablets contain hydrocortisone which is a glucocorticoid.
Glucocorticoids are adrenocortical steroids, both naturally
occurring and synthetic, which are readily absorbed from the
gastrointestinal tract. Hydrocortisone USP is white to practically
white, odorless, crystalline powder with a melting point of about
215 C. It is very slightly soluble in water and in ether; sparingly
soluble in acetone and in alcohol; slightly soluble in chloroform.
INDICATIONS
Endocrine Disorders
Primary or secondary adrenocortical insufficiency (hydrocortisone
or cortisone is the first choice; synthetic analogs may be used in
conjunction with mineralocorticoids where applicable; in infancy
mineralocorticoid supplementation is of particular importance)
Congenital adrenal hyperplasia
Non suppurative thyroiditis
Hypercalcemia associated with cancer
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Rheumatic Disorders
As adjunctive therapy for short-term
administration
(Psoriatic arthritis
Rheumatoid arthritis, including juvenile
rheumatoid arthritis
Ankylosing spondylitis
Acute and subacute bursitis
Acute nonspecific tenosynovitis
Acute gouty arthritis
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Post-traumatic osteoarthritis
Synovitis of osteoarthritis
Epicondylitis
Collagen Diseases
During an exacerbation or as maintenance therapy
in selected cases of:
Systemic lupus erythematosus
Systemic dermatomyositis (polymyositis)
Acute rheumatic carditis
Dermatologic Diseases
Pemphigus
Severe psoriasis
Severe seborrheic dermatitis
Allergic States
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SIDE EFFECTS
Fluid and Electrolyte Disturbances
Sodium retention
Fluid retention
Congestive heart failure in susceptible patients
Potassium loss
Hypokalemic alkalosis
Hypertension
Musculoskeletal
Muscle weakness
Steroid myopathy
Loss of muscle mass
Osteoporosis
Tendon rupture, particularly of the Achilles tendon
Vertebral compression fractures
Aseptic necrosis of femoral and humeral heads
Pathologic fracture of long bones
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DRUG INTERACTIONS
WARNINGS
In patients on corticosteroid therapy
subjected to unusual stress,
increased dosage of rapidly acting
corticosteroids before, during, and
after the stressful situation is
indicated.
Corticosteroids may mask some signs
of infection, and new infections may
appear during their use.
132
PRECAUTIONS
Drug-induced secondary adrenocortical
insufficiency may be minimized by gradual
reduction of dosage.
There
is
an
enhanced
effect
of
corticosteroids
on
patients
with
hypothyroidism and in those with cirrhosis.
Corticosteroids should be used cautiously
in patients with ocular herpes simplex
because of possible corneal perforation.
the reduction should be gradual.
Psychic derangements may appear when
corticosteroids are used.
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CONTRAINDICATIONS
Systemic fungal infections and known
hypersensitivity to components
CLINICAL PHARMACOLOGY
Naturally occurring glucocorticoids
(hydrocortisone and cortisone), which also have
salt-retaining properties, are used as
replacement therapy in adrenocortical deficiency
states. Their synthetic analogs are primarily used
for their potent anti-inflammatory effects in
disorders of many organ systems. Glucocorticoids
cause profound and varied metabolic effects. In
addition, they modify the body's immune
responses to diverse stimuli.
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Vitamin K1 Injection
INDICATIONS
coagulation disorders which are due to
faulty formation of factors II, VII, IX and X
when caused by vitamin K deficiency or
interference with vitamin K activity.
anticoagulant-induced prothrombin
deficiency
prophylaxis and therapy of hemorrhagic
disease of the newborn;
hypoprothrombinemia due to antibacterial
therapy;
hypoprothrombinemia secondary to factors
limiting absorption or synthesis of vitamin 135
Vitamin K1 Injection
Newborns Dosage
Dosage
HemorrhagicDiseaseoftheNewborn
Prophylaxis
0.5to1mgIMwithin1hourofbirth
1mgSCorIM(Higherdosesmaybe
Treatment
Adults
InitialDosage
Anticoagulant-Induced
Prothrombin
2.5 mg to 10 mg or up to 25 mg
Deficiency (caused by coumarin or
indanedionederivatives)
indanedionederivatives)
Hypoprothrombinemia Due to other 2.5mgto25mgormore(rarelyupto
causes(Antibiotics;Salicylates)
50mg)
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SIDE EFFECTS
Deaths have occurred after intravenous and
intramuscular administration.
Transient "flushing sensations" and "peculiar"
sensations of taste have been observed, as well as
rare instances of dizziness, rapid and weak pulse,
profuse sweating, brief hypotension, dyspnea, and
cyanosis.
Pain, swelling, and tenderness at the injection site
may occur.
The possibility of allergic sensitivity
Infrequently, usually after repeated injection,
erythematous, indurated, pruritic plaques have
occurred;
Hyperbilirubinemia
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DRUG INTERACTIONS
Temporary resistance to prothrombin-depressing
anticoagulants may result, especially when larger
doses of phytonadione are used.
If relatively large doses have been employed, it may
be necessary when reinstituting anticoagulant therapy
WARNINGS
Benzyl alcohol as a preservative in Bacteriostatic
Sodium Chloride Injection has been associated with
toxicity in newborns. An immediate coagulant effect
should not be expected after administration of
phytonadione. It takes a minimum of 1 to 2 hours for
measurable improvement in the prothrombin time.
Whole blood or component therapy may also be
necessary if bleeding is severe.
139
PRECAUTIONS
Laboratory Tests
Prothrombin time should be checked
regularly
CONTRAINDICATIONS
Hypersensitivity to any component of
this medication.
140
CLINICAL PHARMACOLOGY
Vitamin K1 Injection (Phytonadione Injectable
Emulsion, USP) aqueous dispersion of
vitamin K1 for parenteral injection,
possesses the same type and degree of
activity as does naturally-occurring vitamin
K, which is necessary for the production via
the liver of active prothrombin (factor II),
proconvertin (factor VII), plasma
thromboplastin component (factor IX), and
Stuart factor (factor X). The prothrombin test
is sensitive to the levels of three of these
four factors-II, VII, and X.
141
II.CARE OF DRUGS:
1. Moisture:
Deliquescent preparations like zinc chloride,ephedrine,
digitalis preparations, ergot preparations must be
preserved from moisture in air tight containers with
dehydrating agents. Nurse must take proper care of
them in their stores during rainy season by keeping
them in dry places.
2. Light:
Direct sun light destroys the activity of drugs. Bismuth
subcarbonate and ephedrine decomposes slowly in
light. Tannic acid, bismuth salts, quinine and
aminopyrine, change their colour with light. These drugs
should be stored in amber or dark colour bottles. Drugs
contained in the colour bottles must be protected from
light by keeping them in dark place.
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3. Temperature:
Biological drugs are damaged even at room
temperature. They must be stored at a
temperature between 2-10C. Small pox vaccine
should be kept even below OC, because of their
losing of potency very rapidly in room
temperature. Biological products, antibiotics, ethyl
nitrite and insulin must be kept in refrigerators (2
15C) in the Drug Stores and Pharmacies and
maintenance of constant low temperature should
be checked.
4.Air:
Air due to 02, CO2, and moisture may cause
deterioration of the drugs. Arsphenamine, chloral
hydrate, calcium lactate, codeine sulphate, ferrous
sulphate, hydantoin sodium, etc. will be damaged
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5. Age:
Arsenic preparations like neoarsphnamine, procaine
solutions, many tinctures, fluid extracts deteriorate with age
in spite of best preservations. Biological drugs and
antibiotics also lose their potency with time. These drugs
should not be sold after the expiration date. These drugs
should be stored separately and constant watch on the
expiry dates of these drugs should be made
6. Bacterial and Fungal growth:
The growth of these plants commonly occur in carbohydrate
containing drugs like syrups and mucilage and also in plant
and animal extracts, and other pharmaceutical preparations
like mixtures, emulsions, ointments, creams,sterile
solutions, injections and biological products.These
preparations may be protected against these growth by
adding 0.2% of benzoic acid Or sodium benzoate and 0.5 %
of chlorbutol, cresol, phenol, sodium bisulphite, etc.
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6. Chemical Stabilizers:
Many drugs which are highly oxidizable such as vitamin C,
adrenaline, phenylephrene, fats and oils are protected by the
use of chemical stabilizers like anti-oxidants such as sodium
bisulphite, sodium meta-bi sulphite maleic acid, or sulphur dioxide. pH sensitive drugs are stabilized by using buffer
solutions. Acetanilide acts as a negative catalyst in hydrogen
peroxide. Sugars are used to prevent decomposition of ferrous
iron in solution.
7. Glass containers:
Glass may also cause deterioration of some drugs.The hard
glass containers contain silicon dioxide which is more resistant
but the soft glass contains sodium and calcium oxides.The soft
glass containers containing solution under high temperature
dissolves the oxides and produces alkaline hydroxides and
increase the pH of the solution and may affect the stability of
the pH sensitive substances.
145
For patients:
It is important to store medicines properly. Guidelines for proper
storage include:
Keep out of the reach of children.
Keep medicines in their original containers.
Store away from heat and direct light.
Do not store capsules or tablets near the kitchen sink, or in other
damp places. Heat or moisture may cause the medicine to break
down. Also, do not leave the cotton plug in a medicine container that
has been opened, since it may draw moisture into the container.
Keep liquid medicines from freezing.
Do not store medicines in the refrigerator unless directed to do so.
Do not leave your medicines in an automobile for long periods of
time.
Do not keep outdated medicine or medicine that is no longer needed.
Be sure that any discarded medicine is out of the reach of children.
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C. Right Dose
Nurse must do:
Calculate and check drug dose accurately.
Check PDR, drug package insert or drug handbook for
recommended range of
specific drugs.
D. Right Time
Nurse must do:
Administer drugs at specified times.
Administer drugs that are affected by foods, before meals.
Administer drugs that can irritate stomach, with food.
Drug administration may be adjusted to fit schedule of clients
lifestyle, &
activities. & diagnostic procedures.
Check expiration date.
Antibiotics should be administered at even intervals.
150
E. Right Route
Nurse must do:
assess ability to swallow before giving oral meds.
Do not crush or mix meds in other substances before
consultation with
physician or pharmacist
Use aseptic technique when administering drugs.
Administer drug at appropriate sites.
Stay with client until oral drugs have been swallowed.
F. Right Assessment
Get baseline data before administration.
Assess the colour of the urine, sweat etc.
Check blood urea , creatinine level for nephrotoxic drugs.
Investigate for liver function if the drug is acting through liver.
Check for any adverse reactions.
151
G. Right Documentation
Immediately record appropriate information
Name, dose, route,time & date, nurses initial or signature
Clients response:
narcotics
analgesics
antiemetics
sedatives
unexpected reactions to medications.
Use correct abbreviations & symbols.
H. Right to Education
Client teaching :
therapeuticpurpose
side-effects
diet restrictions or requirements
skill of administration
laboratory monitoring
Principle of Informed Consent
152
I. Right Evaluation
clients response to medications.
effectiveness
extent of side-effects or any adverse reactions.
J. Right to Refuse
Nurse must do:
determine, when possible, reason for refusal.
explain risk for refusing medications &
reinforce the reason for medication.
Refusal should be documented immediately.
Head nurse or health care provider should be
informed when omission pose
153
155
B. Administration
11. Administer only those drugs that you have
prepared.
12. Identify the client by ID band or ID photo.
13. Offer ice chips when giving bad tasting
medicine.
14. Assist client to appropriate position.
15. Provide only liquids allowed on the diet.
16. Stay with client until meds are taken.
17.Administer no more than 2.5 to 3 ml of solution
by IM at one site.
18.Infants receive no more than 1 ml of solution by
IM at 1 site & no more than 1 ml subcutaneously.
NEVER recap needles.
156
157
159
D. Topical
Applied to skin with a glove, tongue
blade or cotton - tipped applicator.
Apply to clean dry skin when possible.
Do not contaminate the medication in a
container.
Do not double dipped .
Observed sterile technique when skin is
broken.
Use firm strokes if medication is to be
rubbed in.
164
E. Instillations
Eyedrops
1. wash hands
2. lie or seat down and look up towards ceiling
3. remove any discharge by wiping out from inner canthus
4. rest hand holding the dropper against the clients head.
5. gently draw skin down below affected eye to expose
conjunctival sac
6. administer drops into center of the sac
7. gently press lacrimal duct with sterile cotton ball or
tissue for 1 to 2
mins after instillation
8. keep eyes closed for 1 to 2 mins following application
165
Eye Ointment
1, 2, 3, 4,- same as above
5 . squeeze strip of ointment (abt inch, unless stated
otherwise).
5.keep eyes close for 2-3 mins.
6. instruct px for blurred vision for a short time.
7. apply at bedtime, if possible.
Ear Drops
1. wash hands.
2. med shld be at room temp.
3. sit up with head tilted slightly toward unaffected side.
4.child: pull auricle down & back. (after 3yo ,same as adult)
adult: pull up & back
5. instill prescribed drops.
6. do not contaminate dropper.
7. maintain position for 2-3 minutes.
166
Drug Standards:
To predict effect based on consistency,uniform quality
Pure Food and Drug Act (1906) - must be listed in
US Pharmacopeia (USP)
National Formulary (NF)
Drug Laws
Federal Food, Drug, Cosmetic Act (1938)
extensive testing of new drugs
THANK YOU
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