Pmcol Midterm 1
Terms
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- Plasma concentration of a drug is determined by? (3)
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Rate of Absorption
Rate of Elimination: kidney filtration and secretion, biliary secretion, lungs, tears, sweat
Rate of Metabolism: predominantly liver - Drug Binding Sites (4)
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1)Enzymes
2)Carrier Molecules
3)Ion Channels
4)Target Organs - receptors - Receptor Transduction Mechanisms (5)
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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)
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1)cAMP
2)Ca
3)phosphoinositides - Process involved with phosphinositide second messenger activity
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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?
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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
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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)
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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
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1) M and N
2) Rapidly hydrolyzed by acetylcholinesterase and butyrylcholineesterase (pseudcholinesterase) - Characteristics of Methacholine (B methyl acetycholine)
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1) more M than N
2) 3 times more resistant to hydrolysis than acetylcholine - Characteristics of Carbochol (carbamylcholine)
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1) M and N
2) very resistant to hydrolysis - Characteristics of Bethanechol (B methyl carbachol)
- 1) more M than N