Pharma Principles

Question 1

PHASE I DRUG METABOLISM

Answer 1

non synthetic rxn, drug chemically altered and oxidized

Question 2

PHASE II DRUG METABOLISM

Answer 2

synthetic rxn, drug conjugated with another moiety

Question 3

FIRST ORDER ELIMINATION

Answer 3

fraction of drug removed from body is constant and independent of dose.
one half life is 50%, then 75%, 87.5, 93.7, 96.8

Question 4

ZERO ORDER ELIMINATION

Answer 4

amount of drug removed is constant and dependent on dose, generally d/t key enzyme

Question 5

CYP 2D6

Answer 5

codeine -> morphine
poor, intermediate, extensive and ultra rapid metabolizers
PM, IM, EM, UM

Question 6

CYP 3A4

Answer 6

methadone metabolized by CYP 3A4
inhibitors include erythromycin, diltiazem, ketoconozole and saquinavir (increase methadone)
inducers include carbamazepine, phenobarbital, efavirenz, St Johns wort (decrease methadone)

Question 7

NALBUPHINE, BUTORPHENOL

Answer 7

mixed opioid agonists and antagonists

Question 8

RECEPTOR TYPES

Answer 8

• ligand gated ion channels
• g protein coupled signalling
• intrinsic enzymatic activity
• nuclear transcription regulating

Question 9

RECEPTOR DOMAINS

Answer 9

• ligand binding site

- effector/message propagation (signalling) area

Question 10

DRUGS THAT WORK THROUGH

IONOTROPIC RECEPTORS

Answer 10

nicotine
benzodiazepine
phencyclidine
ketamine

Question 11

DRUGS THAT WORK THROUGH

G-i0 RECEPTORS

Answer 11

opioids
cannabinoids
γ-hydroxybutyric acid (GHB)
hallucinogens

Question 12

DRUGS THAT WORK THROUGH

TRANSPORTERS OF BIOGENIC AMINES

Answer 12

cocaine
amphetamine
methamphetamine
NMDA

Question 13

NMDA receptor antagonists

Answer 13

dissociative, hallucinogenic and euphoric

• ketamine
• dextromethorphan (DXM)
• phencyclidine (PCP)
• methoxetamine (MXE)
• nitrous oxide (N20)

Question 14

synthetic opioids NMDAR-antagonists

Answer 14

pethidine
levorphanol
methadone
destropropoxyphene
tramadol
ketobemidone

Question 15

TOLERANCE

Answer 15

pharmacokinetic
pharmacodynamic
learned
conditioned
cross

Question 16

PHARMACOKINETIC TOLERANCE

Answer 16

increased metabolism, less drug available

Question 17

PHARMACODYNAMIC TOLERANCE

Answer 17

adaptive changes in receptor density, efficiency of receptor coupling and/or signal transduction

Question 18

LEARNED TOLERANCE

Answer 18

compensatory mechanisms

Question 19

CONDITIONED TOLERANCE

Answer 19

subset of learned, when specific cues, such as sights, smells or circumstances, to state of expectation.

Question 20

CROSS TOLERANCE

Answer 20

tolerance to specific drug in category is generalized to other drugs in same structural/mechanistic category
eg alcohol, benzos and barbiturates