Pmcol Midterm 1

Front 1

Plasma concentration of a drug is determined by? (3)

Back 1

Rate of Absorption

Rate of Elimination: kidney filtration and secretion, biliary secretion, lungs, tears, sweat

Rate of Metabolism: predominantly liver

Front 2

Drug Binding Sites (4)

Back 2

1)Enzymes
2)Carrier Molecules
3)Ion Channels
4)Target Organs - receptors

Front 3

Receptor Transduction Mechanisms (5)

Back 3

1)Lipid Soluble Ligands
2)Transmembrane receptor enzyme whose internal activity is affected by outside receptor activity
3)As above but stimulates a protein tyrosine kinase
4)Ligand gated ion channel
5)Transmembrane receptor that controls a G-protein

Front 4

Second Messengers(3)

Back 4

1)cAMP
2)Ca
3)phosphoinositides

Front 5

Process involved with phosphinositide second messenger activity

Back 5

1) Cell membrane contains PIP2
2) G protein activates phospholipase C
3) which splits PIP2 to DAG and IP3
4) DAG activates protein kinase C in membrane
5) IP3 goes to cytoplasm and triggers release of Ca

Front 6

Acetylcholine acts at which two receptor sites?

Back 6

1) Muscarinic- activated by muscarine from Amanita muscaria (at all cholinergic receptors except ganglia and neuromuscular junction)

2) Nicotinic- nicotine from tobacco (only at ganglia and NM junctions)

Front 7

Direct-acting Cholinomimetics
(2 subsets)

Back 7

1)Choline esters-acetylcholine, methacholine, carbachol, bethanechol
(all quaternary ammonium, poor abspt)

2)Cholinomimetic alkaloids- muscarine (m), pilocarpine(m), nicotine(n), lobeline(n) *all absorbed good except muscarine, all excreted by kidneys

Front 8

Good and Bad pharmacological effects of direct-acting cholinomimetics

Back 8

1) glaucoma treatment
2) increase AV node of heart
3) exacerbate asthma or COPD
4) diarrhea in high dose
5) voiding of urine
6) nicotine and libeline alerting
->tremor->emesis(vomit)->stimulated respiration->convulsions->coma->death

Front 9

Direct-acting cholinomimetics in use (4)

Back 9

1) Acetylcholine (Miochol) opth
2) Bethanecol (Urecholine) oral and parenteral for GI or Urinary
3) Carbachol (Isopto Carbachol) opth
4) Pilocarpine (Isopto Carpine) opth

Front 10

Characteristics of Acetylcholine

Back 10

1) M and N
2) Rapidly hydrolyzed by acetylcholinesterase and butyrylcholineesterase (pseudcholinesterase)

Front 11

Characteristics of Methacholine (B methyl acetycholine)

Back 11

1) more M than N
2) 3 times more resistant to hydrolysis than acetylcholine

Front 12

Characteristics of Carbochol (carbamylcholine)

Back 12

1) M and N
2) very resistant to hydrolysis

Front 13

Characteristics of Bethanechol (B methyl carbachol)

Back 13

1) more M than N