Adit Faturohman, Dian Purwitasari, Farandy Falach S., Iffa Nadhifa, Khoriah Indri H.

, Mardeleine Priscilla,
Maryam Hanifah M., Minal Lidyawati P., Muthia Salsabila, Nanda Adi K., Nanda Ghaffar , Sefira F.

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Pharmacology
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 1 Drug Interaction
About
with Receptor Site
A neurotransmitter has a specific shape to fit into a receptor site and cause
a pharmacological response such as a nerve impulse being sent. (similar to a
substrate in an enzyme interaction)
After attachment to a receptor site, a drug may either initiate a response or
prevent a response from occurring. A drug must be a close "mimic" of the
neurotransmitter.
An agonist is a drug which produces a stimulation type response. The agonist
is a very close mimic and "fits" with the receptor site and is thus able to initiate
a response.
An antagonist drug interacts with the receptor site and blocks or depresses
the normal response for that receptor because it only partially fits the receptor
site and can not produce an effect. However, it does block the site preventing
any other agonist or the normal neurotransmitter from interacting with the
receptor site.
 About Adverse Drug Reaction
2
• This type of reaction is unpredictable. This is
“A result of drugserious
theraphy but that is neither
affect in lowerintended
number nor expected in
of people
normal therapeutic use and that causes significant, sometimes life-
• Some• adverse
This due drug
to hypersensitivity
reactions are of
not reaction
related or
to the
threatening conditions.” Medical Dictionary, Houghton Miffin
drug's metabolism
therapeutic effect but are usually
• This type •of Example
reaction
predictable, is: desirable
because but
the mechanisms involved are
unavoidable.
Type
largely It1isjaundice,
not serious
understood.
Rashes, but common
anemia, a decrease Type 2 white
in the
• Overdose
Example : Reaction
• Example
blood : cell count, kidneyIdiosyncratic
damage, and nerve Reactions
injury
A person
Stomach that
taking may
a impair
drug
irritation vision blood
to reduce
and bleedingor hearing.
glucose.
occur in people who
regularly
However, use aspirin
the effect of Other
drugs or can
other
Type nonsteroidal
causeof anti-
inflammatory
hypoglycemia, with drugs
symptoms nausea and
Reaction
palpitations
 About Bioavailability
• Physical properties of the drug (hydrophobicity, pKa, solubility)
•“Subcategory of absorption
Whether the formulation and isin athe
is administered fedfraction of an administered
or fasted state
•dose of unchanged
Gastric emptying rate drug that reaches the systemic circulation, one
•of Interactions
the principal with other drugs/foods:
pharmacokinetic properties of drugs”
– Interactions with other drugs (e.g., antacids, alcohol, nicotine)
– Interactions with other foods (e.g., grapefruit juice, pomello, cranberry
juice, brassica vegetables)
Factors Affecting
• Transporters: Substrate of efflux transporters (e.g. P-glycoprotein)
• Health of the gastrointestinal tract
3 Bioavailability
• Enzyme induction/inhibition by other drugs/foods
• Individual variation in metabolic differences
– Age: In general, drugs are metabolized more slowly in fetal, neonatal, and
geriatric populations
• Disease state
– E.g., hepatic insufficiency, poor renal function
T U T O R 12