Medical Pharmacology Ovidius 2014

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Adrenalin epinephrine
Naphazoline
Phenylephrine
Ephedrine
Clonidine
Isoprenaline
Salbutamol
Prazosin
Propranolol

10. Atenolol
11. Labetalol
12. Timolol
13. Atropine
14. Pilocarpine
15. Neostigmine
16. Pirenzepine
17. Ipratropium Bromide

1.
Epinephrine is one of four catecholamines (epinephrine, norepinephrine, dopamine,
and dobutamine) commonly used in therapy. The first three catecholamines occur
naturally in the body as neurotransmitters; the latter is a synthetic compound.
Epinephrine is synthesized from tyrosine in the adrenal medulla and released, along
with small quantities of norepinephrine, into the bloodstream.
a) Pharmacological class : Direct acting Sympathomimetic or Direct acting Adrenergic
Agonist
b) Mechanism of Action : Epinephrine interacts with both and receptors. At low
doses, effects (vasodilation) on the vascular system predominate, whereas at high
doses, effects (vasoconstriction) are strongest.

c) Pharmacologic effects :

I.

II.

III.

IV.

Cardiovascular:
o The major action.
o Strengthens the contractility of the myocardium (positive inotropic action)
o Increases its rate of contraction (positive chronotropic action).
o Cardiac output increases.
o Epinephrine constricts arterioles in the skin, mucous membranes, and viscera and it
dilates vessels going to the liver and skeletal muscle.
o Renal blood flow is decreased.
o Increase in systolic blood pressure, coupled with a slight decrease in diastolic
pressure.
Respiratory:
o powerful bronchodilation by acting directly on bronchial smooth muscle. This action
relieves all known allergic- or histamine-induced bronchoconstriction. In the case of
anaphylactic shock, this can be lifesaving.
o In acute asthmatic attack, epinephrine rapidly relieves the dyspnea.
Hyperglycemia
o significant hyperglycemic effect because of increased glycogenolysis in the liver,
increased release of glucagon and a decreased release of insulin
Lipolysis:
o Epinephrine initiates lipolysis through its agonist activity on the receptors of adipose
tissue

d) Therapeutic uses (indications) :

I.

II.

III.
IV.
V.

Bronchospasm: Epinephrine is the primary drug used in the emergency

treatment of any condition of the respiratory tract when bronchoconstriction has
resulted in diminished respiratory exchange. Within a few minutes after
subcutaneous administration, greatly improve respiratory exchange is observed.
Administration may be repeated after a few hours.
Glaucoma: In ophthalmology, 2% epinephrine solution may be used topically to
reduce intraocular pressure in open-angle glaucoma. It reduces the production of
aqueous humor by vasoconstriction of the ciliary body blood vessels.
Anaphylactic shock: Epinephrine is the drug of choice for the treatment of Type
I hypersensitivity reactions in response to allergens.
Cardiac arrest: Epinephrine may be used to restore cardiac rhythm in patients
with cardiac arrest regardless of the cause.
Anesthetics: Local anesthetic solutions usually contain 1:100,000 parts
epinephrine. The effect of the drug is to greatly increase the duration of the local
anesthesia. It does this by producing vasoconstriction at the site of injection,
thereby allowing the local anesthetic to persist at the injection site before being
absorbed into the circulation and metabolized. Very weak solutions of
epinephrine (1:100,000) can also be used topically to vasoconstrict mucous
membranes to control oozing of capillary blood.

e) Contraindications :
Hypersensitivity
Hypovolemic shock
Coronary insufficiency
Hypertension
f) Adverse Effects :
Anxiety
Headache
Cerebral hemorrhage
Cardiac arrhythmias
Pulmonary edema from pulmonary hypertension

g) Pharmacography : 1 mg/mL IM or subcutaneous, Nasal solution, Oral inhalation

h) Prescription:

Dg/ Asthma attacks

Rp/epinephrine vials 1mg/ml
Nr. I
D.s. subcutaneous 1/3 vial every 84h

a) Pharmacological class : It is a sympathomimetic agent with marked alpha

adrenergic activity
b) Mechanism of Action : Naphazoline is a direct acting sympathomimetic drug, which
acts on alpha-adrenergic receptors in the arterioles of the nasal mucosa. This activates
the adrenal system to yield systemic vasoconstrction. In producing vasoconstriction, the
result is a decrease in blood flow in the nasal passages and consequently decreased
nasal congestion. The vasoconstriction means that there is less pressure in the
capillaries and less water can filter out, thus less discharge is made.

c) Pharmacologic effects : induce systemic vasoconstriction, thereby decreasing nasal

congestion and inducing constriction around the conjunctiva. The sympathomimetic
action constricts the smaller arterioles of the nasal passages, producing a decongesting
effect. Ophthalmic use causes constriction of blood vessels in the eyes. It also
decreases itching and irritation of the eyes. Constricts the vascular system of the
conjunctiva. It is presumed that this effect is due to direct stimulation action of the drug
upon the alpha adrenergic receptors in the arterioles of the conjunctiva resulting in
decreased conjunctival congestion.
d) Therapeutic uses (indications) : Naphazoline is primarily indicated in conditions like
Corneal vascularity, Hyperaemia, Itching, Nasal congestion, and can also be given in
adjunctive therapy as an alternative drug of choice in Sinusitis

e) Contraindications : In narrow angle glaucoma or in persons with hypersensitivity

f) Adverse Effects :
Ocular : severe hypertensive crisis, Mydriasis, irritation, keratitis, lacrimation, redness,
increased intraocular pressure
Systemic : Dizziness, Headache, nausea , sweating, weakeness, nervousness, cardiac
irregularities, hyperglycemia
g) Pharmacography : Ophthalmic drops 0,1% , Nasal drops

h) Prescription

Dg/Rhinitis
Rp/Naphazoline sol 0.1%
Nr. I
D.s. Externally 1 drop intranasal 3times/day

a) Pharmacological class : is a direct-acting, synthetic adrenergic agonist

b) Mechanism of Action : Binds primarily 1 receptors. 1-adrenergic receptors mediate
contraction and hypertrophic growth of smooth muscle cells. Phenylephrine produces its
local and systemic actions by acting on 1-adrenergic receptors peripheral vascular
smooth muscle. Stimulation of the 1-adrenergic receptors results in contraction
arteriolar smooth muscle in the periphery. Phenylephrine decreases nasal congestion by
acting on 1-adrenergic receptors in the arterioles of the nasal mucosa to produce
constriction; this leads to decreased edema and increased drainage of the sinus
cavities.
c) Pharmacologic effects : Phenylephrine is a vasoconstrictor that raises both systolic
and diastolic blood pressures. It has no effect on the heart itself but rather induces reflex
bradycardia when given parenterally. Also causes pulmonary vessel constriction and
subsequent increase in pulmonary arterial pressure. Vasoconstriction in the mucosa of
the respiratory tract leads to decreased edema and increased drainage of sinus cavities.
d) Therapeutic uses (indications) : It is often used topically on the nasal mucous
membranes and in ophthalmic solutions for mydriasis. It is mainly used to treat nasal
congestion, but may also be useful in treating hypotension and shock, hypotension
during spinal anaesthesia, prolongation of spinal anaesthesia, paroxysmal
supraventricular tachycardia, symptomatic relief of external or internal hemorrhoids, and
to increase blood pressure as an aid in the diagnosis of heart murmurs. Decreases
edema and increased drainage of sinus cavities.
e) Contraindications : Hypertention
f) Adverse Effects :Large doses cause hypertensive headache and cardiac irregularities.
g) Pharmacography :
i. Syrup 1,25mg/ 0.8ml
ii. supository,
iii. opth. Drops,
iv. Tablets 10mg-20mg
v. IV: 0.2-0.5 mg/dose
vi. IM or subcutaneous: 2 to 5 mg every 1 to 2 hours as needed.,
vii. oint., cream
h) Prescription

Dg/ Hypotension
Rp/Phenylephrine vial 10mg/ml
Nr. I
D.s. IV vial rapidly

4.

a) Pharmacological class : Mixed action Adrenergic agonist OR mixed-acting

symphatomimetic agent( with both, direct and indirect actions).

b) Mechanism of Action : direct and indirect actions on the adrenergic receptor system,
which is part of the sympathetic nervous system. Ephedrine increases post-synaptic
noradrenergic receptor activity by (weakly) directly activating post-synaptic -receptors
and -receptors, but the bulk of its effect comes from the pre-synaptic neuron being
unable to distinguish between real adrenaline or noradrenaline from ephedrine. The
ephedrine, mixed with noradrenaline, is transported through the noradrenaline reuptake
complex and packaged (along with real noradrenaline) into vesicles that reside at the
terminal button of a nerve cell. Ephedrine's action as an agonist at most major
noradrenaline receptors and its ability to increase the release of both dopamine and to a
lesser extent, serotonin by the same mechanism is presumed to have a major role in its
mechanism of action.

c) Pharmacologic effects :
a. Its primary action is indirect- it causes the release of NE from storage in nerve
terminals, apparently by competing with NE for transport into granules.
Second- it produces direct stimulation of adrenergic R.
b. In IV administration it has the same effects with epinephrine , the pressor
response occurs more slowly and lasts 10 times longer.
c. Its potency is 1/250 that of epinephrine in producing an equivalent pressor
response.
d. Increase peripheral resistance and cause cardiac stimulation
e. Bronchodialation
f. Its causes CNS stimulation: insomnia, nervousness, nausea, agitation.
g. Tachyphylaxis with repeated administration.

d) Therapeutic uses (indications) : Ephedrine commonly used as a stimulant, appetite

suppressant, concentration aid, decongestant, and to treat hypotension associated with
anaesthesia.

e) Contraindications : Ephedrine should not be used in conjunction with certain

antidepressants. Ephedrine should be used with caution in patients with inadequate fluid
replacement , impaired adrenal,
function, hypoxia, hypercapnia, acidosis,hypertension, hyperthyroidism, prostatic
hypertrophy, diabetes mellitus, cardiovascular disease, during delivery if maternal BP >
130/80 mmHg, and lactation, closed angle glaucoma, phaeochromocytoma asymmetric
septal hypertrophy, tachyarrhythmias or ventricular fibrillation, hypersensitivity to
ephedrine or other stimulants.

f) Adverse Effects :
o Cardiovascular: tachycardia, cardiac arrhythmias, angina
pectoris, vasoconstriction with hypertension
o Dermatological: flushing, sweating, acne vulgaris
o Gastrointestinal: nausea
o Genitourinary: decreased urination due to vasoconstriction of renal arteries. Also,
difficulty urinating is not uncommon, as alpha-agonists such as ephedrine constrict the
internal urethral sphincter, mimicking the effects of sympathetic nervous system
stimulation.
o Nervous system: restlessness, confusion, insomnia, mild
euphoria, mania/hallucinations (rare except in previously existing psychiatric
conditions),delusions, formication (may be possible, but lacks documented
evidence) paranoia, hostility, panic, agitation
o Respiratory: dyspnea, pulmonary edema
o Miscellaneous: dizziness, headache, tremor, hyperglycemic reactions, dry mouth

g) Pharmacography : Oral :Tablet, capsule 25mg, powder Injectable : IV and IM

h) Prescription
Dg/Rhinitis
Rp/Ephedrine sol. 1%
Nr. I
D.s. intranasally 2 drops per nosetrill 2
times / day for 1 week

5.
a) Pharmacological class : 2 Direct Acting Adrenergic Agonist
b) Mechanism of Action :
Clonidine treats high blood pressure by stimulating 2-receptors in the brain, which
decreases peripheral vascular resistance, lowering blood pressure. It has specificity
towards the presynaptic 2-receptors in the vasomotor center in the brainstem. This
binding decreases presynaptic calcium levels, thus inhibiting the release
of norepinephrine (NE). The net effect is a decrease in sympathetic tone.
Its mechanism of action in the treatment of ADHD is to increase noradrenergic tone in
the prefrontal cortex (PFC) directly by binding to postsynaptic 2 adrenergic
receptors and indirectly by increasing norepinephrine input from the locus coeruleus.
c) Pharmacologic effects :
Decreases presynaptic calcium levels, thus inhibiting the release of norepinephrine (NE)
Decreases peripheral vascular resistance, lowering blood pressure
d) Therapeutic uses (indications) : Used to treat high blood pressure, Attention deficit
hyperactivity disorder, anxiety/panic disorder, and certain pain conditions. Clonidine may
be used to ease withdrawal symptoms associated with the long-term use of narcotics,
alcohol and nicotine (smoking). It can alleviate opioid withdrawal symptoms by reducing
the sympathetic nervous system response such as tachycardia and hypertension, as
well as reducing sweating, hot and cold flashes, and general restlessness. Also can be
used for severe Dysmenorrhea
e) Contraindications : hypersens. to drug/class/component,coagulation disorder (epidural
use), anticoagulant use (epidural use), avoid abrupt withdrawal, caution in elderly pts
caution if cardiovascular dz or severe CAD or if recent MI or cardiac conduction
disturbance or if renal impairment or if depression or if cerebrovascular dz or caution if
CNS depressant use or alcohol use
f) Adverse Effects :
Very common : Dizziness ,Orthostatic hypotension , Dry mouth, Headache (dosedependent), Fatigue, Skin reactions (if given transdermally), Hypotension
Common : Anxiety, Constipation, Sedation (dose-dependent), Nausea/vomiting,
Malaise Weight gain/loss
Uncommon: Delusional perception, Hallucination, Nightmare, Paraesthesia, Sinus
bradycardia, Raynaud's phenomenon, Pruritus (itchiness), Urticaria (hives)
g) Pharmacography : Epidural inj., patch 0.2mg, tablet 0.2mg-0.4mg
h) Prescription
Dg/ ADHD
Rp/Clonidine, patch 0.2mg
Nr. XXX
D.s. Dermal placement, 1 per day

6.

a) Pharmacological class : It is a non-selective beta-adrenergic agonist

b) Mechanism of Action : Isoproterenol is a direct-acting synthetic catecholamine that
predominantly stimulates both b1- and b2-adrenergic receptors. Its nonselectivity is one of
its drawbacks and the reason why it is rarely used therapeutically. Its action on alpha
receptors is insignificant.

c) Pharmacologic effects :
o Cardiovascular: Isoproterenol produces intense stimulation of the heart to increase
its rate and force of contraction, causing increased cardiac output. It is as active as
epinephrine in this action and, therefore, is useful in the treatment of atrioventricular
block or cardiac arrest. Isoproterenol also dilates the arterioles of skeletal muscle (2
effect), resulting in decreased peripheral resistance. Because of its cardiac
stimulatory action, it may increase systolic blood pressure slightly, but it greatly
reduces mean arterial and diastolic blood pressure.
o

Pulmonary: A profound and rapid bronchodilation is produced by the drug.

Isoproterenol is as active as epinephrine and rapidly alleviates an acute attack of
asthma when taken by inhalation (which is the recommended route). This action
lasts about 1 hour and may be repeated by subsequent doses.
Other effects: Other actions on receptors, such as increased blood sugar and
increased lipolysis, can be demonstrated but are not clinically significant.

d) Therapeutic uses (indications) : Isoproterenol is now rarely used as a broncho-dilator in

asthma. It can be employed to stimulate the heart in emergency situations.

e) Contraindications : Isoprenaline should not be administered to patients with myocardial

ischemia. Cardiac arrest was noted in several instances
f) Adverse Effects :

Anxiety
Headache
Cerebral hemorrhage
Cardiac arrhythmias
Pulmonary edema from pulmonary hypertension

g) Pharmacography : IM , spray, sol, gel

h) Prescription
Dg/Athma
Rp/Isoprenaline , MDI 80g
Nr. I
D.s. inhalatory 1 puff every 8h / 7days

7.
a) Pharmacological class : short-acting, selective 2-adrenergic receptor agonist
b) Mechanism of Action : it stimulates 2-adrenergic receptors. Binding of the drug to 2
receptors in the lungs results in relaxation of bronchial smooth muscles. It Inhibits the
phosphorylation of myosin and lowers intracellular calcium concentrations. A lowered
intracellular calcium concentration leads to a smooth muscle relaxation and
bronchodilation. In addition to bronchodilation, salbutamol inhibits the release of
bronchoconstricting agents from mast cells, inhibits microvascular leakage, and
enhances mucociliary clearance.

c) Pharmacologic effects : Being 2 agonists they have a relaxing effect on bronchial

smooth muscle and show little effect on cardiac 1- cardiac R
c) Therapeutic uses (indications) : bronchial asthma, bronchospasm, COPD
d) Contraindications : sensitivity to drug, are not recommended for acute asthma
e) Adverse Effects :
i. regular use of short-acting beta 2 agonists can be associated with
increased bronchial hyperresponsiveness to methacoline challenge
ii. tolerance
iii. caution in patients with CV disease or hyperthyroidism, because they can
have minimal effects on 1 R of the heart.
iv. Tremor, due to stimulation of skeletal muscle
f) Pharmacography : Respiratory as aerosols inhalants, but also are available as oral
powder and solution.Oral: Liquid sol and tab. IM and IV sol.

g) Prescription :

Dg/Asthma
Rp/Salbutamol MDI 90g
Nr. I
D.s. inhalatory, 1 puff when needed no
more than 8puffs per day

a) Pharmacological class : selective 1- adrenergic antagonist

b) Mechanism of Action : Acts by inhibiting the postsynaptic 1-adrenoceptors on
vascular smooth muscle. This inhibits the vasoconstrictor effect of circulating and locally
released catecholamines (epinephrine and norepinephrine), resulting in peripheral
vasodilation.
c) Pharmacologic effects :

Reduces vascular tone in both resistance and capacitance vessels

Because it has no effect on 2-R, neurotransmitter feed-back inhibition is maintained,
so that it causes only a small degree of tachycardia
It decreases arterial pressure with little change in cardiac output, heart rate and right
atrial pressure

d) Therapeutic uses (indications) :

Mild-moderate hypertension
Congestive heart failure
Symptomatic benign prostatic hyperplasia

e) Contraindications :
Hypersensitivity to drug/class/component
caution in elderly pts
caution if cataract surgery

f) Adverse Effects :

First dose effect = postural hypotension; to avoid this effect doses are increased
slowly, till the therapeutic dose, and the first minimal dose to be administered in the
evening.

g) Pharmacography : Oral caps and tablets 5mg

h) Prescription
Dg/Hypertension
Rp/Prazosin tab. 5mg
Nr.XXX
D.s. orally 1cap/day for 30 days

a) Pharmacological class: Sympathetic antagonist.

b) Mechanism of action: non-selective blocker. Propanolol blocks stimulation of 1adrenergic (myocardial) and beta2-adrenergic (pulmonary, vascular and uterine) receptor
sites. This action decreases cardiac output, slows heart rate and reduces blood pressure.

c) Therapeutic use:

- Hypertension, often combined with a diuretic

- Prophylaxis of angina pectoris
- Prophylaxis of supra and ventricular arrhythmias
- Long-term prophylaxis in patients who have had myocardial infarction and are at high risk
for infarction or sudden death
- Management of hypertrophic cardiomyopathies to reduce the force of myocardial
contractions
- Management of hyperthyroidism and anxiety states to decrease the heart rate
- Prophylaxis of migraine headaches

d) Pharmacologic effects :
- It decreases the heart rate and cardiac output and prolongs systole.
- It decreases total coronary blood flow and oxygen consumption
- It reduces blood flow to most tissues, except to the brain
- It inhibits the renal secretion of renin.
- It depresses Na+ excretion, because it alters renal hemodynamics
- It increases airway resistance by 2 blockade
- It interfere with carbohydrate and fat metabolism

e) pharmacography and modality of administration:

Oral: Tablet 40mg , capsule 40mg

Intravenous: solution.
f) Adverse effects:
- It can induce heart failure
- Rapid withdrawl can lead to supersensitivity= up-regulation, of -adrenergic R, which
can provoke anginal attacks, arrhythmias or myocardial infarction
- Cautions in asthmatics and in diabetic patients treated with insulin, or persons with
hypoglycemia
- Rash, fever, purpura
- Prolong use: fatigue, depression, nightmares, sexual disfunctions, peripheral arterial
insufficiency
- C-I in patients with Raynaud syndrome
g) Contraindications:
o Reversible airways disease, particularly asthma or COPD.
o Bradycardia (<60 beats/minute)
o Sick sinus syndrome
o Atrioventricular block (second or third degree)
o Shock and Severe hypotension

h) RP/

Dg/Hypertension
Rp/Propranolol tab. 40mg
Nr. LX
D.s. orally 1tab/12h for 30 days

a) Pharmacological class: Sympathetic antagonist

b) Mechanism of action: Selective 1 receptor antagonist. Developed as a remplacement for
propranolol in the treatment of hypertension. Atenolol competes with sympathomimetic
neurotransmitters for binding at 1adrenergic receptors in the heart and vascular smooth muscle,
inhibiting sympathetic stimulation--> reduction in resting heart rate, cardiac output, systolic and
diastolic blood pressure, and reflex orthostatic hypotension.
c) Therapeutic use:
o Hypertension.
o Prophilaxis of angina pectoris.
o Long-term prophylaxis in patients who have had myocardial infarction and are at
high risk for infarction or sudden death
o Prophilaxis of supraventricular and ventricular tachycardia.
o Grave's disease until antithyroid medication can take effect.
d) Pharmacologic effects:
o It decreases the heart rate and cardiac output and prolongs systole.
o It decreases total coronary blood flow and oxygen consumption
o It inhibits the renal secretion of renin.
o It depresses Na+ excretion, because it alters renal hemodynamics
e) Pharmacography and modality of administration: Tablets 50mg-25mg , I.V Injection
f) Adverse effects: Unlike propranolol, atenolol does not pass through the bloodbrain barrier
thus avoiding various central nervous system side effects.
o Type II diabetes.
o indigestion, constipation, dry mouth
o dizziness or faintness, fatigue, weakness, lack of energy
o impotence
o rhinitis
o depression
o confusion
o insomnia, nightmares
o Edema
g) Contraindications: atenolol should not be provided to patients with:
avoid abrupt withdrawal
caution if peripheral vascular disease, bronchospastic disease, diabetes mellitus,
thyroid disorder, renal impairment, pregnancy and breastfeeding
8. RP/
Dg/Hypertension
Rp/Atenolol tab 50mg
Nr. XXX
D.s. orally 1tab/day for 30 days

a. Pharmacological class: sympathetic antagonist

b. Mechanism of action: non-selective beta-blocker with alfa1 blocking activity. Labetolol
blocks stimulation of beta1-adrenergic (myocardial) and beta2-adrenergic (pulmonary,
vascular and uterine) receptor sites. This action decreases cardiac output, slows heart
rate and reduces blood pressure.
c. Therapeutic use: Used to treat mild to severe hypertension. It reduces peripheral
resistance while preventing reflex tachycardia. It has a particular indication in the
treatment of pregnancy-induced hypertension (pre-eclamsia)
d. Pharmacologic effects: The action on both 1 (relaxation of arterial smooth muscle
and vasodilation) and Rs (1 blockade contributes to a fall in blood pressure in part
by blocking reflex SY stimulation of the heart) contribute to the fall in blood pressure.
e.

Pharmacography and modality of administration:

o Avaiable in oral: Tablet 100-200mg, for therapy of chronic hypertension.
o Avaiable as i.v. sol 100/200mg per 20/40ml vial For hypertensive emergencies.

f.

Adverse effects: it can cause postural hypotension and jaundice.

g. contraindications: asthma, congestive heart failure, any degree of heart block,

bradycardia, hypotension or cardiogenic shock.

8. RP/
Dg/Chronic Hypertension
Rp/Labetalol tab. 100mg
Nr.XXX
D.s. orally, 1 per 24h for 30 days

a) Pharmacological class: Sympathetic antagonist.

b) Mechanism of action: A non-selective beta blocker. blocks stimulation of beta1-

adrenergic (myocardial) and beta2-adrenergic (pulmonary, vascular and uterine) receptor

sites. This action decreases cardiac output, slows heart rate and reduces blood pressure
(depresses renin secretion).

c) Therapeutic use:

to treat high blood pressure.

To treat glaucoma
to prevent heart attacks
to prevent migraine headaches
to treat high intraoqular pressure

d) Pharmacologic effects: - It reduces aqueous humour production through blockage of the

beta receptors on the ciliary epithelium and thus intraoqular pressure. Also Decreases
cardiac output, slows heart rate and reduces blood pressure
e) Pharmacography and modality of administration:
Oral: tablet.10mg
Ophthalmic: liquid, solution 0.25%-0,5%, solution drops

f) Adverse effects:
The most serious possible side effects include cardiacarrhythmias and severe bronchospasms.
Timolol can also lead to fainting, congestive heart failure, depression,confusion, worsening of
Raynaud's syndrome and impotence.
g) Contraindications:
o caution if peripheral vascular dz
o caution if bronchospastic dz
o caution if major surgery
o caution if diabetes mellitus
o caution if thyroid disorder
o caution if WPW syndrome
o caution if pheochromocytoma
o caution if renal impairment
o caution if hepatic impairment
o caution if pregnancy 2nd or 3rd trimester
o caution if myasthenia gravis
8. RP/
Dg/Glaucoma
Rp/Timolol ophthalmic sol. 0.25%
Nr.I
D.s. conjuctivally 2 drops in each
conjuctival sac for 10 days

a) Pharmacological class: Cholinergic antagonist, antimuscarinic agent.

b) Mechanism of action:Has a high affinity for muscarinic receptors, where it binds
competitively, preventing acetylcholine from binding to those sites. Atropine acts both
centrally and peripherally.
c) Therapeutic use:Ophthalmic: permits measurement of refractive errors without the
interference of accomodative capacity of the eye.
Antispasmodic: relax GIT and bladder.
Antidote for cholinergic agonists: used for treatment of overdoses of insecticides.
Antisecretory: blocks secretions in upper and lower respiratory tracts prior to
surgery.
d) Pharmacologic effects: Its general actions last about 4 hours except when placed
topically in the eye, where the action may last for days.
Eye: persistent mydriasis, unresponseviness to light.
Gastrointestinal: reduces activity of GIT.
Urinary system: reduces hypermotility states of urinary bladder.
Cardiovascular: depending on the dose:
low doses: bradycardia
higher doses: the cardiac rate increases modestly.
Antisecretory: blocks salivary, sweat and lacrimal glands.

e) Pharmacography and modality of administration:

Ophthalmic: liquid, ointment, solution.
Oral: liquid, solution/drops, tablet
Intramuscular injection.
Intravenous injection.
f) Adverse effects:

Dry mouth, blurred vision, tachycardia, constipation.

CNS: restlessness, confusion, hallucinations, delirium, depression.

Collapse of circulatory and respiratory system.

g ) Contraindications:
glaucoma, acute angle-closure
obstructive uropathy
paralytic ileus
toxic megacolon
asthma
myasthenia gravis
caution in elderly pts
caution if high environmental temperature
8. RP/

Dg/Uveitis
Rp/Atropine ophth sol 1%
Nr.I
D.s. Instill 1 drop in each conjuctival sac
for 7 days

a) Pharmacological class: direct acting cholinergic agonists

b) Mechanism of action: Cholinergic parasympathomimetic agent that stimulates
muscarinic receptors, increasing secretion by the exocrine glands, and producing
contraction of the iris sphincter muscle and ciliary muscle (when given topically to the
eyes).

c) Therapeutic use: Use in both narrow angle and wide angle glaucoma.
d) Pharmacologic effects:
o topically in cornea:
miosis and spasms of accomodation of eye.
Impossibility to foccus vision.
Increased drainage of aqueous humor.
o
Secretory: stimulation of sweat, tears, saliva.
e) Pharmacography and modality of administration:
Ophthalmic: gel, liquid, solution.
Oral: liquid, solution, drops, tablet.
f) Adverse effects: Pilocarpine can enter the brain and cause CNS disturbances.
It stimulates profuse sweating and salivation.
g) Contraindications:

cardiovascular diseases.
Respiratory diesases.
Hepatic impairment.
Psychiatric disorder.

8. RP/

Dg/Glaucoma
Rp/Pilocarpine ophth. Sol 1%
Nr.I
D.s. conjuctivally 2 drops in each
conjuctival sac for 30 days

a) Pharmacological class: Indirect-acting cholinergic agonists.

b) Mechanism of action: Neostigmine is a parasympathomimetic, specifically, a reversible
cholinesterase inhibitor. The drug inhibits acetylcholinesterase which is responsible for
the degredation of acetylcholine. So, with acetylcholinesterase inhibited, more
acetylcholine is present By interfering with the breakdown of acetylcholine, neostigmine
indirectly stimulates both nicotinic and muscarinic receptors which are involved in
muscle contraction.. It does not cross the blood-brain barrier.

c) Therapeutic use: used in symptomatic treatment of myasthenia gravis.

Used to stimulate bladder and GIT.
Used as an antidote for tubocurarine and other competitive neuromuscular
blocking agents.

d) Pharmacologic effects:
reversibly inhibits acetylcholinesterase.
Stimulates contractility of skeletal muscle.

e) Pharmacography and modality of administration:

Intramuscular: liquid.
Intravenous: liquid.
Oral: tablet.15mg

f) Adverse effects:salivation, flushing, decreased blood pressure, nausea, abdominal

pain, diarrhea and bronchospasm.

g) Contraindications: Contraindicated in patients with known hypersensitivity to the drug,

patients with peritonitis or mechanical obstruction of the intestinal or urinary tract.

8. RP/

Dg/ Myasthenia gravis

Rp/Neostigmine tab. 15mg
Nr.XXX
D.s. orally 2 tabs per day for 15 days

a) Pharmacological class: Antimuscarinic agent.

b) Mechanism of action: Muscarinic receptor antagonist that binds to the muscarinic
acetylcholine receptor.

c) Therapeutic use:

Treatment of peptic ulcer, gastric ulcer and duodenal ulcer.

Prophylaxis of duodenal ulcer recurrence.
Relieves cramps or spasms of the stomach, intestines and bladder.
Prevents nausea, vomiting and motion sickness.

d) Pharmacologic effects:
It reduces gastric acid secretion.
It reduces muscular spasms.

e) Pharmacography and modality of administration:

Tablets 25mg

f) Adverse effects:
Dry mouth, blurred vision, drowsiness, dizziness, nausea or loss of appetite,
diarrhea, constipation, bitter taste, decreased sexual ability or desire, bad breath

g) Contraindications: Renal failure

8. RP/

Dg/Peptic ulcer
Rp/Pirenzepine tab 25mg
Nr. LX
D.s. orally 1 tab per 24h for 30days, 30
mins before food

a) Pharmacological class : nonselective muscarinic antagonist

b) Mechanism of Action :
Ipratropium bromide is an anticholinergic agent. It blocks muscarinic cholinergic
receptors, without specificity for subtypes, resulting in a decrease in the formation of
cyclic guanosine monophosphate (cGMP). Most likely due to actions of cGMP on
intracellular calcium, this results in decreased contractility of smooth muscle.
c) Pharmacologic effects : Decreased contractility of smooth muscle in the lung,
inhibiting bronchoconstriction and mucus secretion. Hypersensitivity to atropine and
related substances.
d) Therapeutic uses (indications) :
For maintenance treatment of bronchospasm associated with chronic obstructive
pulmonary disease, including chronic bronchitis and emphysema.
e) Contraindications : narrow angle glaucoma and obstructions in the gastrointestinal
tract and urinary system

f) Adverse Effects : Dry mouth and sedation have been reported. Also, effects such as
skin flushing, tachycardia, acute angle-closure glaucoma, nausea, palpitations and
headache have been observed. Inhaled ipratropium does not decrease mucociliary
clearance. The inhalation itself can cause headache and irritation of the throat in a few
percent of patients. Urinary retention has been reported in patients receiving doses by
nebulizer. As a result, caution may be warranted, especially by in men with prostatic
hypertrophy.
g) Pharmacography : Nasal Spay or aerosol, respiratory solution

h) Prescription
Dg/Asthma
Rp/IPRATROPIUM BROMIDE MDI 18g
Nr. I
D.s. inhalatory 1 puff 3 times per day for
14days