Term
| What drugs exhibit zero-order elimination (concentration doesn't affect rate of elimination)? |
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Definition
Phenytoin, Ethanol and Aspirin
PEA (a pea is round, shaped like a 0 for "zero-order") |
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Term
| What is the difference between Phase I and II metabolism of drugs? |
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Definition
I = P450, yields polar, water-soluble metabolites (reduction, oxid, hydrolysis)
II = conjugation, yields very polar, inactive metabolites
Geriatric pts lose phase I first! |
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Term
| How do competitive and noncompetitive inhibitors affect Km and Vmax? |
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Definition
Competitive = Vmax same, Km higher = decreased potency (lower affinity...lower Km = higher affinity)
Noncompetitive = Km same, Vmax lower = decreased efficacy |
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Term
| How does potency change with a partial agonist? |
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Definition
Can change either way (up or down)...it's a separate variable
Partial agonists only decrease maximal effect (decreased efficacy) |
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Term
| Do safer drugs have a high or low Therapeutic Index? |
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Definition
| Safe drugs = higher TI (LD50/ED50) |
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Term
| What G-protein receptors are associated with Gq? What 2nd messenger does Gq use? |
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Definition
PLC/IP3
HAVe 1 M&M
H1 (allergy), Alpha-1, V1 (vascular), M1 (CNS, ENS) and M3 (everything but CNS and heart) |
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Term
| What G-protein receptors are associated with Gs? What 2nd messenger does Gs use? |
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Definition
cAMP (activates AC)
B1, B2, D1 (renal), H2 (gastric acid) and V2 (aquaporins) |
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Term
| What G-protein receptors are associated with Gi? What 2nd messenger does Gi use? |
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Definition
cAMP (inhibits AC and decreased cAMP)
alpha-2, M2 (heart) (M4), D2
MAD 2's |
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Term
| What drug blocks choline uptake into the nerve terminal and effectively blocks ACh synthesis? |
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Definition
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Term
| What drug blocks ACh transport into vesicles? |
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Definition
| Vesamicol (VESicles and ChOl) |
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Term
| What activates the release of ACh from nerve terminal vesicles? What inhibits it? |
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Definition
Ca activates
Botulinum inhibits |
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Term
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Definition
| Depletes cathecholamines in adrenergic terminals --> blocks them getting into vesicles so they are susceptible to MAO degradation |
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Term
| What drugs induce NE release from nerve terminals? |
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Definition
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Term
| What drugs block reuptake of NE at the pre-syn nerve terminal? |
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Definition
Cocaine, TCAs and amphetamine
Effectively increased NE in the synapse |
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Term
| What anticholinesterase is NOT used for the CNS? Which is used for the eys? |
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Definition
NOT CNS = Neostigmine
Eyes = Physostigmine (PHYS is for the EYES) |
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Term
| What class of drugs don't you want to give to pts w/ asthma, COPD or peptic ulcers? |
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Definition
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Term
| What is the effect of organophosphates? |
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Definition
Inhibit acetylcholinesterase. Causes DUMBBELSS
Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Excitation of skeletal muscle and CNS, Lacrimation, Sweating and Salivation
Tx w/ atropine and Pralidoxime |
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Term
| What drug is an AChE reactivator? |
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Definition
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Term
| What muscarinic antagonist is used for Parkinson's? |
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Definition
| Benztropine (PARK my BENZ) |
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Term
| What muscarinic antagonist is used for Asthma and COPD? |
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Definition
Ipratropium
I PRAy I can breathe soon! |
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Term
| What are the side effects of atropine? |
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Definition
Muscarinic antagonist (adrenergic effects)
Hot as a hare (no sweating), Dry as a bone, Red as a beet, Blind as a bat (no accomodation), Mad as a hatter
Can cause acute angle-closure glaucoma! |
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Term
| Dobutamine affects what adrenergic receptors? |
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Definition
beta-1 > beta-2
Inotropic but not chronotropic |
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Term
| Phenylephrine is used for what? What does it do? |
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Definition
Pupillary dilation, vasocontriction and nasal decongestion
alpha-1 > alpha-2 stimulation |
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Term
| What are the selective Beta-2 agonists? |
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Definition
| Albuterol (short acting), Salmeterol (long acting), Terbutaline (reduce premature uterine contractions) |
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