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Pmcol Midterm 1


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

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

Rate of Metabolism: predominantly liver
Drug Binding Sites (4)
2)Carrier Molecules
3)Ion Channels
4)Target Organs - receptors
Receptor Transduction Mechanisms (5)
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
Second Messengers(3)
Process involved with phosphinositide second messenger activity
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
Acetylcholine acts at which two receptor sites?
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)
Direct-acting Cholinomimetics
(2 subsets)
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
Good and Bad pharmacological effects of direct-acting cholinomimetics
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
Direct-acting cholinomimetics in use (4)
1) Acetylcholine (Miochol) opth
2) Bethanecol (Urecholine) oral and parenteral for GI or Urinary
3) Carbachol (Isopto Carbachol) opth
4) Pilocarpine (Isopto Carpine) opth
Characteristics of Acetylcholine
1) M and N
2) Rapidly hydrolyzed by acetylcholinesterase and butyrylcholineesterase (pseudcholinesterase)
Characteristics of Methacholine (B methyl acetycholine)
1) more M than N
2) 3 times more resistant to hydrolysis than acetylcholine
Characteristics of Carbochol (carbamylcholine)
1) M and N
2) very resistant to hydrolysis
Characteristics of Bethanechol (B methyl carbachol)
1) more M than N

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