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34 Cards in this Set

  • Front
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phenobarbital, MTX, TCA, ASA...
tx OD with what? why?
bicarb. These drugs are weak acids, and become trapped in basic environments.
Tx OD of amphetamines w/ what? Why?
Ammonium chloride. The amphetamines are weak bases, and become trapped (and excreted) in acidic environments.
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.
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
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
What is the mechanism of Muscarinic ACh receptors? Types?
G-protein-coupled that act thru second messengers. M1-5.
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
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
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.
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))
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.
Carbachol class/mech.
- uses?
Cholinomimetic agent used for glaucoma, pupillary contraction, and release of intraocular pressure.
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!"
Methacholine class/mech
- uses?
Cholinomimetic: stim muscarinic receptors in airway when inhaled.
- challenge test for asthma dx.
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.
Drug of choice for urinary retention?
Bethanechol
Edrophonium class and use.
Indirect cholinergic agonist --> inhibits AChE.

- used to diagnose myasthenia gravis ...it's VERY short acting.
Echothiophate class and use?
AChE inhibitor.

Glaucoma.
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)
What is Pralidoxime?
prompts regeneration of active AChE.

given with atropine for anti-AChE OD.
Atropine class?
- organ system affects?
- application?
muscarinic antag
eye
produce mydriasis and cycloplegia (paralysis of ciliary muscle ---> loss of accomodation)
homatropine class?
- organ system affects?
- application?
muscarinic antag
eye
produce mydriasis and cycloplegia (paralysis of ciliary muscle ---> loss of accomodation)
tropicamide class?
- organ system affects?
- application?
muscarinic antag
eye
produce mydriasis and cycloplegia (paralysis of ciliary muscle ---> loss of accomodation)
Benztropine class?
- organ system affects?
- application?
Muscarinic antagonist
- CNS
- Parkin' my Benz (Parkinson's dz)
Scopolamine class?
- organ system affects?
- application?
M antag
- CNS
- motion sickness
Ipratroprium class?
- organ system affects?
- application?
Muscarinic antag
- Respiratory
- Asthma, COPID ("[I pra]y I can breathe soon")
Oxybutynin class?
- organ system affects?
- application?
Muscarinic antag
- Genitourinary
- Reduces urgency in mild cystitis and reduces bladder spasms.
Glycopyrrolate class?
- organ system affects?
- application?
Muscarinic antag
- Genitourinary
- Reduces urgency in mild cystitis and reduces bladder spasms.
Methscopolamine class?
- organ system affects?
- application?
Muscarinic Antag
- GI
- PUD tx
pirenzepine class?
- organ system affects?
- application?
Muscarinic Antag
- GI
- PUD tx
Propantheline class?
- organ system affects?
- application?
Muscarinic antag
- GI
- PUD tx.
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"
Atropine can cause what in the elderly?
- men w/ prostatic hyperplasia?
- infants?
acute angle-closure glaucoma in the elderly.
- urinary retention
- hyperthermia.
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.