semester 1 Flashcards
Pharmacokinetics
study of how the body affects the drug
4 phases
Absorption
Distribution
Metabolism
Excretion
Law of mass action
states that the rate of chemical reactions I proportional to the concentration of reacting substances
D+R=DR RT=R+DR
Emax model
Emax{D}/EC50+{D}
Therapeutic index
TC50/EC50
Pharmacological effect
depends on:
active molecule reaching active site
adequate conc at the active site
Enteral administration
drug administration via the GI tract e.g.
oral,rectal,sublingual,buccal,nasogastric,nasojejunal,gastrostomy and jejunostomy
Enteral factors
Concentration Lipid solubility
Formulation Molecular size
Gastric contents Blood supply
GI tract
consists of mouth, oesophagus, stomach, intestines and anus
First pass metabolism
when a drug administered via enteral route travels to the liver and its concetration decreases before it reaches systemic circulation
Parenteral administration
administration by any other than via Gi tract e.g.
intramuscular(90),intravenous(20),subcutaneous(45), intradermal(5-10)
Bioavailability(F)
Its the fraction of drug which reaches systemic circulation unchanged, Iv has a an F of 1/100%
ER-some lost due to first pass metabolism,
F=AUC oral/AUC Iv
Bioavailability(F) factors
1)Drug factors 2)Patient factors
Concentration Blood supply
Formulation Motility
Molecular size Absorption surface
Gastric content
Bile
Formulation
the process where different chemical substances including the active drug are combined to give a medicinal product
Active ingredient
any component of active drug that intends to furnish pharmacological activity
Drug product
finished dosage for e.g. tablet
Active transport
movement of substances against a concentration gradient from an area of low con to an area of high conc, using ATP
Facilitated diffusion
movement of substances down a conc gradient using a carrier protein
Pinocytosis
cells engulf liquid droplets by forming vesicles
Diffusion
movement of substances down a concentration gradient
Weak acids
Proton donors
HA–>H++A-
Weak bases
proton acceptors
B+H+–>BH+
Pka
50% ionised, 50% unionised (drug)
Ka=[H][Weak base]/[weak acid]
pH=pka+log(A/HA) pr pH=pka+log(B/BH)
Topical administration
1) Local effect- drug applied to the localised area on body surface to prevent systemic side effects ( creams, ointments, sprays and drops)
2) Systemic effect- drug applied to the body surface to provide an alternative route into blood (nicotine patch)