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34 Cards in this Set
- Front
- Back
phenobarbital, MTX, TCA, ASA...
tx OD with what? why? |
bicarb. These drugs are weak acids, and become trapped in basic environments.
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Tx OD of amphetamines w/ what? Why?
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Ammonium chloride. The amphetamines are weak bases, and become trapped (and excreted) in acidic environments.
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Phase I drug metabolism?
Phase II? Which do geriatric pts lose first? |
P450, involveds reduction, oxidation, hydrolysis, etc. Metabolite often STILL ACTIVE.
Conjucation (-ation)... --> INACTIVE metabolite. Type I. |
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Follow a parasympathetic nerve from origin until the messages gets to the target.
Sympathetic? |
Comes down from CNS --> NICOTINIC synapse onto 2nd cell body --> MUSCARINIC synapse onto target.
I. NICOTINIC synapse DIRECTLY onto Adrenal medulla II. NICOTINIC synapse in sympathetic chain --> 1. MUSCARINIC onto sweat glands 2. NE (a, B) onto cardiac/smooth/ gland, nerve terminals 3. D1 = Renal vascular smooth muscle |
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What types of receptors are Nicotinic Ach receptors?
- two types and places they're found? |
ligand gated Na/K channels
- N(n) i/ autonomic ganglion - N(m) i/ NMJ |
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What is the mechanism of Muscarinic ACh receptors? Types?
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G-protein-coupled that act thru second messengers. M1-5.
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Three G protein types and their mechanisms.
Give the important types of each. |
Gi --> INHIBITS Adenyl cyclase --> \\cAMP --> \\PKA
Gs --> ^^AC --> ^^cAMP (from ATP) --> ^^PKA Gq --> Phospholipase C --> (converts lipids to) PIP2 --> 1. IP3 --> ^^Ca 2. DAG --> ^^PKC "HAVe 1 M&M" = G(q) (exiciting too) - H1, a1, V1, M1, M3 "B.B.D.H.V. = Bring Back 'Dat Hum-Vee!" - B1, B2, D1, H2, V2 "MAD 2's" = G(i) - M2, a2, D2 |
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Where do the following drugs inhibit Cholinergic neurotransmission?
- Hemicholium - Vesamicol - Botulinum |
- inhibits choline reuptake into presynaptic terminal
- inhibits ACh repackaging into vesicles - inhibits presynaptic ACh vesicle release |
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Where do the following drugs modify Noradrenergic neurotransmission?
- Metyrosine - Reserpine - Guanethidine - Amphetamine (2 ways!) - Cocaine, TCAs |
- inhibits Tyrosine conversion into DOPA.
- inhibits Dopamine packaging/conversion into NE. - Inhibits NE vesicle fusion/release - INCREASES NE vesicle release, and INHIBITS NE reuptake. - INHIBITS NE reuptake. |
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Which receptors at the noradrenergic nerve terminal provide for inhibition of NE release caused by a signal?
Upregulates release? What is the receptor for the local NE negative feedback mechanism? |
M2 (thru G(i))
Ang II a2 (via G(i)) |
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Drug used for postoperative or neurogenic ileus, as well as urinary retention?
- mechanism? |
Bethanechol
- Cholinomimetic: activates bowel and bladder smooth muscle, and is resistant to AChEsterase. |
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Carbachol class/mech.
- uses? |
Cholinomimetic agent used for glaucoma, pupillary contraction, and release of intraocular pressure.
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Pilocarpine class/mech.
- uses? |
Cholinomimetic: stimulates contraction of ciliary muscle of eye (open angle), pupillary sphincter (narrow angle) --> resistant to AChE.
- STIMULTATION of sweat, tears, and saliva. "Pile on the Sweat and Tears!" |
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Methacholine class/mech
- uses? |
Cholinomimetic: stim muscarinic receptors in airway when inhaled.
- challenge test for asthma dx. |
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What is the mechanism of the -stigmine's?
- use of Neostigmine? - use of Physostigmine? - Pyridostigmine? |
Indirect choline agonists (inhibit AChE)
- postop and neurogenic ileu, urinary retention, myasthenia gravis, reversal of NMJ blockade after surgery. Does NOT penetrate BBB. - Glaucoma (crosses BBB-->CNS) and atropine OD. - longer acting form of Physostigmine. Does NOT penetrate CNS/BBB. |
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Drug of choice for urinary retention?
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Bethanechol
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Edrophonium class and use.
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Indirect cholinergic agonist --> inhibits AChE.
- used to diagnose myasthenia gravis ...it's VERY short acting. |
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Echothiophate class and use?
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AChE inhibitor.
Glaucoma. |
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Sx of anti-AChE poisoning?
- antidote? |
Way to much autonomic stim for you:
- Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Excitiation of skeletal muscle and CNS, Lacrimation, Sweating, and Salivation. - Atropine (blocks muscarinic receptors) + pralidoxime (chemical antagonist used to regenerate active cholinesterase) |
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What is Pralidoxime?
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prompts regeneration of active AChE.
given with atropine for anti-AChE OD. |
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Atropine class?
- organ system affects? - application? |
muscarinic antag
eye produce mydriasis and cycloplegia (paralysis of ciliary muscle ---> loss of accomodation) |
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homatropine class?
- organ system affects? - application? |
muscarinic antag
eye produce mydriasis and cycloplegia (paralysis of ciliary muscle ---> loss of accomodation) |
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tropicamide class?
- organ system affects? - application? |
muscarinic antag
eye produce mydriasis and cycloplegia (paralysis of ciliary muscle ---> loss of accomodation) |
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Benztropine class?
- organ system affects? - application? |
Muscarinic antagonist
- CNS - Parkin' my Benz (Parkinson's dz) |
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Scopolamine class?
- organ system affects? - application? |
M antag
- CNS - motion sickness |
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Ipratroprium class?
- organ system affects? - application? |
Muscarinic antag
- Respiratory - Asthma, COPID ("[I pra]y I can breathe soon") |
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Oxybutynin class?
- organ system affects? - application? |
Muscarinic antag
- Genitourinary - Reduces urgency in mild cystitis and reduces bladder spasms. |
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Glycopyrrolate class?
- organ system affects? - application? |
Muscarinic antag
- Genitourinary - Reduces urgency in mild cystitis and reduces bladder spasms. |
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Methscopolamine class?
- organ system affects? - application? |
Muscarinic Antag
- GI - PUD tx |
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pirenzepine class?
- organ system affects? - application? |
Muscarinic Antag
- GI - PUD tx |
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Propantheline class?
- organ system affects? - application? |
Muscarinic antag
- GI - PUD tx. |
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Pt just took a drug that was supposed to decrease their urinary urgency. Now, they've got increased body temp, rapid pulse, dry mouth, dry flushed skin, cycloplegia, constipation, disorientation.
- drug? |
atropine.
"Hot as a hare Dry as a bone Red as a Beet Blind as a Bat Mad as a hatter" |
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Atropine can cause what in the elderly?
- men w/ prostatic hyperplasia? - infants? |
acute angle-closure glaucoma in the elderly.
- urinary retention - hyperthermia. |
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Hexamethonium class and uses?
- toxicities? |
Nicotinic antag
- blocks ganglion --> used to help prevent vagal reflex responses to changes in BP - severe orthostatic hypotension, blurred vision, constipation, sexual dysfunction. |