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32 Cards in this Set

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P-450 Inducers
Queen Barb Steals Phen-phen and Refuses Greasy Carbs CHRONICally
- Quinidine (both induction/inhibition)
- Barbiturates
- St. John's Wart
- Phenytoin
- Rifampin
- Griseofulvin
- Carbamazepine
- CHRONIC alcohol use
P- 450 Inhibitors
INHIBIT yourself from drinking a KEG because it makes you ACUTEly SICk
- Ketoconazole
- Erythromycin
- Grapefruit juice
- ACUTE alcohol use
- Sulfonamides
- INH
- Cimetidine
adrenoreceptors
alpha 1 (vascular sm mm, sphincters, dilatory mm in eye)
alpha 2 (decrease symp outflow)
beta 1 (myocytes)
beta 2 (myocytes, uterus, periphery)
G proteins:
q (increased ca2+ intracelluarly, increased PKC)
i (decreased cAMP, PKA)
s (increased cAMP, PKA)
s
muscarinic receptors
M1 (CNS, enteric system)
M2 (heart)
M3 (exocrine glands, bladder, bronchioles, ciliary mm)
G proteins
q (increase Ca2+ in cell, increased PKC)
i (decrease cAMP, PKC)
q
dopamine receptors
D1 (vascular sm mm)
D2 (transmitter release in brain)
G proteins
s (increase cAMP, PKA)
i (decreased cAMP, PKA)
histamine receptors
H1 (resp; involved in pain)
H2 (gastric acid secretion)
G proteins
q (increase Ca2+ in cell, PKC)
s (increase cAMP, PKA)
Vasopressin
V1 (vascular sm mm)
V2 (kidney)
G proteins
q (increased Ca2+ in cell, PKC)
s (increase cAMP, PKA)
Name the 6 major direct-acting cholinomimetic agents
1. Acetylcholine (prototype)
2. Bethanechol
3. Carbachol
4. Pilocarpine
5. Methacholine
6. nicotine
Name the 6 major indirectly acting cholinomimetic agents
1. Isofluorphate
2. Echothiophate
3. Parthion
4. Edrophonium
5. Physotigmine
6. Neostigmine
What's the difference between a direct and an indirect cholinergic agonist?
Direct = binds/activates the muscarinic/nicotinic receptors

Indirect = inhibits AChE to increase the total amt of ACh in the synapse
What are the 2 major families of cholinergic receptors?
1. Muscarinic
(M1-M3 in ganglia, sm mm, sec. glands, myocardium, CNS)

2. Nicotinic
(Nn, Nm in autonomic ganglia and NM jxn)
What are the organophosphates?
What classic symptoms do they cause?
Name the 3 in use today.
1. Indirect cholinergic agonist (bind AChE)
2. DUMBBELSS
3. isofluorate, echothiphate, parathion
What are cholinergic antagonists?
bind cholinergic receptors (both M and N) without trigger usual downstream response
What are the 3 subclasses of cholinergic antagonists?
1. Muscarinic Blockers
2. NM blockers
3. Ganglionic Blockers
What are the 6 major muscarinic antagonists?
1. Atropine (prototype)
2. Scopolamine
3. Homatropine
4. Cyclopentolate
5. Tropicamide
6. Pirenzepine
What are some other drugs with antimuscarinc properties?
1. benztropine (Parkinson's)
2. antidepressants (chlorpromazine)
3. antihistamines (diphenhydramine)
4. antiasthmatics (ipratropium)
What are the toxic effects of atropine?
Dry mouth (dry as a bone)
anhydrosis (hot as a hare)
tachycardia/cutaneous vasodilation (red as a beet)
blurred vision (blind as a bat)
hallucinations/delirium (mad as a hatter)
What are adrenergic agonists?
drugs/catecholamines that activate adrenergic receptors (alpha and beta receptors)

AKA sympathomimetics
What are some important alpha-selective direct-acting adrenergic agonists?
1.Phenylephrine
2. methoxamine
3. clonidine
4. methyldopa
What are some important beta-selective direct-acting adrenergic agonists?
1. Dobutamine (unstable CHF, shock)
2. Isoproterenol (Heart block, bradycardia)
3. Albuterol
4. Metaproterenol
5. Terbutaline (prevention of premature labor)
Name 2 indirect-acting adrenergic agonists.
1. Tyramine
2. amphetamine
Name 2 mixed (both direct and indirect) adrenergic agonists.
1. ephedrine
2. metaraminol
what are adrenergic antagonists?
drugs that bind to, but don't activate, the alpha and beta adrenergic receptors
What are the (7) alpha adrenergic blockers?
1. Prozosin
2. Doxazosin
3. Terazosin (above 3 = HTN, urinary retention in BPH)
4. Phenoxybenzamine (NONREVERSIBLE), used for pheo
5. Tamsulosin (BPH)
6. Yohimbine (erectile dysfunction)
7. Phentolamine (pheo)
What are the B1-selective blockers? (4)
1. atenolol
2. esmolol
3. acebutolol (partial agonist)
4. metoprolol
What are some important B2-selective blockers?
1. propranolol
2. timolol
3. nadolol
What's the advantage of using a B1 selective blocker?
They don't cause the bronchoconstrictive and hypoglycemic effects of nonselective beta blockers
what are some beta blockers with alpha blocking capacity?
1. labetalol - allows peripheral vasodilation in HTN and atrial fib
2. Carvediolol - for chronic CHF and HTN
What is an important B2 selective blocker?
butoxamine (no current clinical use)
What are indirect adrenergic antagonists?
they block release of NE from nerve endings and antagonize effects of the sympathetic nervous system
What are the two important indirect adrenergic antagonists?
Guanethidine (binds to storage vesicles)

Reserpine (blocks NE transport from cytoplasm into vesicles)

Both used very rarely to treat HTN
If you weren't studying for boards, what would you be doing right now?
use your imagination....

and remember to smile :)