DRUGS Flashcards
Are low molecular weight chemical substances that interact with macromolecular targets in the body to produce effect.
DRUGS
what the drug does to the body
pharmacodynamics
- Body’s own natural chemicals
-
within
➢ Ex. Neurotransmitters, hormones, autacoids
endogenous compounds
- Foreign substances such as drugs (Xenobiotics)
- outside
exogenous compounds
drug is powerful and selective ; select this part when designing a drug
therapeutic
drug is less powerful.
subtherapeutic
drugs is less selective
toxic
what the body does to the drug
pharmacokinetics
k - katawan
GOAL: Design a drug that will interact as powerfully and selectively as possible for the target
pharmacodynamics
GOAL: Design a drug so that it is capable of reaching that target
pharmacokinetics
Dictates the fate or destiny of the drug (ADME)
Absorption
Distribution
Metabolism
Excretion
pharmacokinetics
- also called Liberation
- extract and get the API away from excipient and dissolve (drug in aqueous solution) – pre-requisite for drug absorption.
Drug Release
process of drug entry into the systemic circulation ; wherein the drug in the GI tract will now proceed to the bloodstream
Absorption
main site for absorption
small intestine
main site of metabolism
liver
drug will be distributed to different organs and tissues (possess proteins and nucleic acids)
Distribution
composed of processes metabolism (chemical reaction that makes the drug inactive) and excretion (functional loss of the drug from the body)
Elimination
organ responsible for excretion
kidney
the most common mechanism controlling drug release.
Diffusion
- Extract API from dosage form and done via dissolution process— aqueous solution.
- When the conventional dosage forms are administered orally or topically, the active drug in the dosage form is immediately released and absorbed into the systemic circulation.
Liberation
➢ Most complicated route due to numerous barriers
➢ GIT
➢ The most common and popular route
Oral administration
tasks of organs that could transmit the drug to enter the blood.
absorption environment
ABSORPTION ENVIRONMENT
❖ both have acidic and basic environment.
❖ pH 1.5-2 fed state (more production and release of hydrochloric acids)
❖ pH 2-6 fasting state
STOMACH
ph level of fed state in stomach
1.5 - 2
ph level of fasting state in stomach
2 - 6
ABSORPTION ENVIRONMENT
❖ main site of absorption
❖ basic environment
❖ anatomical feature is high surface area because of the presence of villi and microvilli.
❖ greater perfusion
small intestine
Drug is absorbed if it is
LUNA
Lipophilic (cell membrane is lipophilic; like dissolves like)
Unionized
Non-polar
Drug is excreted if it is
HIPE
Hydrophilic
Ionized
Polar
Drugs are weak ____
electrolytes
weak acids
weak bases
acid + acid
basic + basic
unionized, absorbed
acid + basic
basic + acid
ionized, excreted
TRUE OR FALSE
A weakly basic drug is absorbed in the small intestine because it exists in its lipophilic, unionized, and polar formed
FALSE - non polar
➢ Less complication
➢ Direct to Systemic Circulation
➢ Rapidly distributed
➢ IV, IM, SC, Intraspinal, Intracerebral
Parenteral administration
➢ Protects the brain from exposure to chemicals and metabolites, due to the presence of tightly joined epithelial cells lining the cerebral capillaries
➢ Lipophilic
Blood Brain Barrier
Higher perfusion, ____ distribution
higher
- Delivery of drug to the tissue is controlled by the specific blood flow to a given tissue.
- Drug delivery to the target site
Perfusion
Chemical conversion of drugs to make them inactive → HIPE
Biotransformation
DRUG METABOLISM
All substances in the circulatory system, including drugs, metabolites, and nutrients, will pass through the
liver
are agents that are initially inactive and become active via metabolism
prodrug
- Pre-systemic metabolism
- Reduction of bioavailability = subtherapeutic
- a significant proportion of a drug is metabolized by hepatic enzymes during the initial trip through the liver
- Drug removal by the liver after absorption
First-pass effect
➢ stimulate → enhance
➢ ↑ IA
➢ increased metabolism, ↓ Concentration in plasma
Enzyme induction
induce
➢ decreased metabolism, ↑ Concentration in plasma
Enzyme inhibition
drug reenters the intestinal tract from the liver through bile duct
Enterohepatic recirculation
➢ Bile acid
➢ Reabsorption of bile acid
➢ Drugs such as Oral contraceptive pills
Biliary recycling
EXCRETION
➢ Most abundant
➢ Majority of drugs are ____ excretion
urine / urinary
EXCRETION | RENAL CLEARANCE
unbound (free) drug is passively
filtered by the glomerulus
Glomerular Filtration
EXCRETION | RENAL CLEARANCE
drug is actively secreted → urine
tubular secretion
EXCRETION | RENAL CLEARANCE
drug is passively reabsorbed back into the blood
Tubular reabsorption