Sei sulla pagina 1di 13

I.

INTRODUCTORY MATERIAL

●Drug Definitions
● Acid-Base Chemistry
DRUG DEFINITIONS
● Drug: Any substance that causes an alteration or modification of a biological
process.
Therefore, penicillin, ethanol, arsenic and carbon monoxide all are drugs.
Several of these are considered “poisons” by laypersons. However, all
poisons are drugs and all drugs have the potential to be poisonous, i.e.,
produce adverse effects. Any drug can produce adverse effects if it is
administered in sufficiently high doses (as described by Paracelsus almost
500 years ago, see Figure I-1) and by an appropriate route of administration.
● Chemical Name: The scientific name of the drug that describes its molecular
structure.
● Generic Name: A simple drug name that is often the legal name of the drug.
● Brand or Trade Name: The name assigned to a specific drug formulation for
marketing purposes by the manufacturer. The product may contain more than
a single pharmacologically active agent as well as specific additives. These
names include both prescription and non-prescription (over the counter or
OTC) drugs.
● Street Name: The name(s) of a drug used by users and abusers.
Examples of drug names

● Chemical name: 5-allyl-5-(1-methyl)barbituric acid


Generic name: Secobarbital
Brand name: Seconal
Street name: Black beauties

● Chemical name: (5, alpha-6,alpha)-7,8-Didehydro-4,


5-epoxy-17-methylmorphinan-3,6-diol diacetate
Generic name: Heroin, Diacetylmorphine
Brand name: not legal in the Malaysia
Street name: H, Smack, Horse

● Chemical name: 7-chloro-1,3-dihydro-1-methyl-5-phenyl-2H-1,4


Generic name: Diazepam
Brand name: Valium
Street name: Vallies
DRUG SPECIALISTS

● Pharmacologist: A scientist who studies the effects produced by


drugs and the mechanisms by which those effects are produced.
● Toxicologist: A scientist who studies the adverse effects
produced by drugs and the mechanisms by which those adverse
effects are produced.
● Medicinal or Pharmaceutical Chemist: A scientist who studies
the chemical characteristics of drugs including their biochemical
effects, synthesis and structure activity relationships.
● Pharmacist: A scientist licensed by the state to compound and
dispense drugs.
● Physicians, psychiatrists, and nurses: Have expertise
concerning the drugs required in their practices to diagnose and/or
treat diseases.
● Drug abusers: Abusers may have some expertise as to certain
aspects of drug effects and methods of detection.
DRUG EFFECTS

● Local Effects: Effects that are produced at the site of administration.


● Systemic Effects: Effects that are produced at a site other than the
site of application.
● Therapeutic Effects: The effects of a drug that are used to diagnose
or treat a disease or syndrome
● Disease: an interruption, cessation or disorder of body functions,
systems or organs, i.e., a sickness or illness.
● Syndrome: The group of signs and symptoms associated with a
disease.
● Sign: An abnormality discoverable or observable by the physician or
other observer, e.g., rash, glucose.
● Symptom: An abnormal condition experience by the patient, e.g.,
nausea, - a subjective characteristic.
● Side Effects: All of the effects, other than the therapeutic effects,
produced at therapeutic doses.
● Toxic Effects: The effects produced when greater than therapeutic
doses are used.
DOSES

● Dose: The amount of drug administered


● Effective Dose (ED): The dose required by a specific route of administration
to produce a specific effect.
● Therapeutic Dose (ThD): The dose required by a specific route of
administration to produce a desired therapeutic effect.
● Toxic Dose (TD): The dose required by a specific route of administration to
produce a toxic effect.
● Lethal Dose (LD): The dose required by a specific route of administration to
produce death.
● Quantitative effective doses: Due to biological/genetic variation, there is
not a single ED for an entire population. Therefore, ED is expressed as the
dose, by a specific route of administration required to produce the desired
effect in a specific % of the tested population. The therapeutic (ThD), toxic
(TD) or lethal dose (LD) in any % of a population, e.g., ThD12, TD 99 or LD25.
● A common (and somewhat outdated) measure of drug safety is the
Therapeutic Index (TI). The TI = LD50 / ED50.
● Potency: A relative measure of the doses of 2 or more drugs required to
produce a specific effect by a specific route of administration, i.e., a
comparison of effective doses.
DRUG ACTION

● Pharmacodynamic actions or Pharmacological effects: The effects that a


drug produces in a biological system.
● Structurally Non-specific Drugs: Drugs whose action is dependent
primarily not on their structures, but on their physical characteristics.
● Structurally Specific Drugs: Drugs whose action is dependent primarily on
their structures.
● Target Molecules: Molecules with which structurally specific drugs interact
to produce effects.

DRUG INTERACTIONS

● Addition or Summation: The combined effect of two or more drugs used


together is the sum of the effects of each drug used separately.
● Synergism or Potentiation: The combined effect of two or more drugs used
together is greater than the sum of the effects of the drugs when they are used
together, i.e., a greater than additive effect
● Antagonism: The combined effect of two or more drugs used together is less
than the sum of each drug used separately.
TOLERANCE AND ADDICTION

● Tolerance: The phenomenon by which following the repeated administration


of a drug, a dose larger than the initial dose is required to produce the initial
effect.
● Pharmacokinetic or Dispositional Tolerance: Tolerance caused by an
alteration in one or more aspects of disposition.
● Pharmacodynamic or Functional Tolerance: Tolerance caused by an
alteration in the response of the target molecule to the drug.
● Addiction: The phenomenon by which the abrupt discontinuance of drug use
leads to the production of symptoms.
● Negative Drug Reinforcement: The drive that causes a person to use a drug
in order to prevent the occurrence of adverse effects associated with the
cessation of use.
● Positive Drug Reinforcement: The drive that causes a person to use a drug
in order to continue experiencing the desirable effects of the drug.
ACIDS/BASES DEFINITIONS

Arrhenius definitions
Acids : substances that produce hydrogen ions in water solution
HA H+ + A -

Bases : substances that produce hydroxide ions in water solution


BOH B+ + OH-

Lewis definitions
Describes behavior in non-protonic systems
Acid - donates pair of electrons
Base - accepts pair of electrons
:NH3 + BF3 H3N:BF3
ACIDS/BASES DEFINITIONS

Bronstead and Lowry definitions


Acids: Substances that can yield a proton in water solution
HA H+ + A -
Bases : Substances that can accept a proton in water solution
B + H+ BH+

Better representation
HA + H20 H3O+ + A-
acid base conj conj
acid base

B + H20 BH+ + OH-


base acid conj conj
acid base
DISSOCIATION OF ACIDS AND BASES

Dissociation of a weak acid


HA + H20 H3O+ + A-
dissociation constant of a weak acid = Ka
Ka = [A- ] [H3O+ ]
[HA] [ H2O]
pKa = the negative log of the acid dissociation constant

Dissociation of the conjugate base


A- + H20 HA + OH-
dissociation constant of a weak base = Kb
Kb = [OH- ] [HA]
[A-] [ H2O]
pKb = the negative log of the base dissociation constant

Dissociation constant of water


the dissociation constant of water = Kw = (Ka)(Kb)
pKw = 14 at 25° C; 14.96 at 0° C; 13.26 at 50° C
RELATIVE STRENGTH OF ACIDS AND BASES

usually both Ka and pKa are given for weak acids and weak bases
● for weak acids, the values are for the acids
● for weak bases, the values are for their conjugate acids

Stronger acids have


● larger Ka values
● smaller pKa values
e.g.
acid #1 with a Ka of 10-3 and pKa of 3
acid #2 with a Ka of 10-8 and pKa of 8

Stronger bases have


smaller Ka values
larger pKa values
e.g.
base #1 with a Ka of 10-10 (Kb of 10-4) and pKa of 10 (pKb of 4)
base #2 with a Ka of 10-3 (Kb of 10-11) and pKa of 3 (pKb of 11)
EFFECT OF pH ON DISSOCIATION OF ACIDS AND BASES
 
The Henderson-Hasselbach equation
allows degree of ionization of acids and bases to be determined at various pH
values
for weak acids
pH = pKa + log [A-] , at equilibrium
[HA]

If pH < pKa, then [HA] > [A-]


If pH > pKa, then [HA] < [A-]

for weak bases


pH = pKa + log [B] , at equilibrium
[BH+]

If pH < pKa, then [B] > [BH+]


If pH > pKa, then [B] < [BH+]

Potrebbero piacerti anche