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236 Cards in this Set
- Front
- Back
MUSCARINIC 1 RECEPTOR (M1)
|
-neural
-increases IP3 & DAG |
|
MUSCARINIC 2 RECEPTOR (M2)
|
-cardiac (SA & AV nodes)
-increases K efflux and decreases cAMP -result: decrease HR |
|
MUSCARINIC 3 RECEPTOR (M3)
|
-glandular
*smooth muscle & glands: increases IP3 & DAG -->sm. m. contraction & glandular secretion *vascular sm. m.: increases cGMP (via NO stimulation from Arg) --> Sm. m. relaxation -->VD (**Erection) |
|
nicotinic receptors in muscle
|
-at NM Jxn. -->Na influx -->depolarization
--> muscle contraction |
|
nicotinic receptors in neurons
|
-in autonomic ganglia
-->Na influx --> excitation of postganglionic neurons |
|
muscarinic agonistic effects
|
eye: tear,PC, accomidation
Heart: decrease HR, increase PR interval, M3=VD Rs: BC ***do not give to asthamtics or COPD pts. GI/GU: increase contraction/motility |
|
choline esters
list physical characteristics absorption distribution |
ACh, Bethanechol, Carbachol
+ charged quaternary ammonium compounds poor GI absorption No CNS distribution |
|
reversible anticholinesterases
list MOA physical characteristics |
-Donepezil, Tacrine
-Edrophonium: + charge quaternary alcohol; prevents ACh hydrolysis (does not prevent binding to AChE) -Neostigmine, Physostigmine, Pyridostigmine: carbamic acid esters; competes with ACh for binding site on AChE physostigmine=tert amine; good absorption in GI; penetrates BBB; neo & pyridostigmine=quat. amine; less GI absorption; no BBB crossing |
|
Irreversible anticholinesterases
list physical characteristics MOA uses |
Echothiophate, Isoflurophate, Malathion
organophosphates (pesticides): esters of phosphoric acid lipid soluble=good absorption through any body part (SKIN) covalent bond at AChE cat. site; aging=hydrolysis=stronger bond |
|
symptoms & treatment of organophosphate poisoning
|
-"DUMBBELSS"=Diarrhea, Urination, miosis, Bronchospasm, Bradycardia, exciitation of sk.m., lacrimation, sweating, salivation
-cardio & Rs support -use cholinergic antagonist (ex Atropine) to block excessive ACh -pralidoxine (2-PAM) to regenerate AChE (must do early b/c more difficult to displace anti-AChE after "aging") |
|
ACETYLCHOLINE
|
cholinergic receptor agonist
-choline ester -binds muscarinic & nicotinic |
|
ACETYLCHOLINE
admin & use |
-admin: intraocular
-use: miosis (PC=pupillary constriction) during ophthalmic surgery -admin: intracoronary -use: coronary angiography: VD & Vasospasm to Dx vasospastic angina |
|
BETHANECHOL
|
-direct cholinergic agonist
-choline ester -binds muscarinic receptors |
|
BETHANECHOL
admin & use |
admin: oral or subcutaneous
use: postop or postpartum urinary & ileus retention ***no effect on HR or BP b/c does binds muscarinic receptors only |
|
CARBACHOL
|
-direct acting cholinergic agonist
-choline ester -binds muscarinic & nicotinic |
|
CARBACHOL
admin & uses |
admin: topical ocular
use: glaucoma COAG: activates ciliary muscle NAG: activates pupillary sphincter admin: intraocular use: PC durin ophthalmic surgery |
|
MUSCARINE
|
-direct cholinergic receptor
-plant alkaloid (poisonous mushrooms--> D, sweating, salivation, tearing) -selectively activates muscarinic receptor |
|
MUSCARINE
admin & uses |
none
|
|
NICOTINE
|
-direct cholinergic agonist
-plant alkaloid -selectively activates nicotinic receptor |
|
NICOTINE
admin & uses |
admin: oral or transdermal
uses: smoking cessation |
|
PILOCARPINE
|
-direct cholinergic agonist
-plant alkaloid (tert. amine) -activates muscarinic > nicotinic |
|
PILOCARPINE
admin & uses |
admin: topical ocular
use: glaucoma COAG: activates ciliary muscle NAG: activates pupillary sphincter admin: oral use: xerostomia (dry mouth) |
|
DONEPEZIL
|
-Indirect cholinergic agonist
-reversibly inhibits cholinesterase |
|
DONEPEZIL
admin, DOA, use |
admin: oral
DOA: 1 day use: Alzheimer's |
|
EDROPHONIUM
|
-indirect cholinergic agonist
-reversibly inhibits cholinesterase |
|
EDROPHONIUM
admin, DOA, use |
admin: IV
DOA: 10 min use: diagnose MG |
|
NEOSTIGMINE
|
-indirect cholinergic agonist
-reversibly inhibits cholinesterase |
|
NEOSTIGMINE
admin, DOA, use |
Admin: oral, subQ, IM
use: MG, postop urinary/ileus retention & abdominal distention admin: IV use: antidote for curariform drug toxicity DOA: 2-4 hrs. |
|
PHYSOSTIGMINE
|
-indirect cholinergic agonist
-reversibly inhibits cholinesterase |
|
PHYSOSTIMINE
admin, DOA, use |
admin: topical ocular
use: COAG admin: IM/IV use: reverse CNS effects of antimuscarinic drugs (ex. Atropine overdose) DOA: 1-5 hrs. |
|
PYRIDOSTIGMINE
|
-indirect cholinergic agonist
-reversibly inhibits cholinesterase |
|
PYRIDOSTIGMINE
admin, DOA, use |
admin: oral, IM, IV
use: MG admin: IV use: antidote for curariform drug toxicity DOA: 3-6 hrs. |
|
TACRINE
|
-indirect cholinergic agonist
-reversibly inhibits cholinesterase |
|
TACRINE
admin, DOA, use |
Admin: oral
DOA: 4-6 hrs. use: Alzheimers |
|
ECHOTHIOPHATE
|
-indirect cholinergic agonist
-irreversibly inhibits cholinesterase |
|
ECHOTHIOPHATE
admin, DOA, use |
admin: topical ocular
DOA: 1+ wks use: COAG & strabismus (accomodative esotropia) |
|
ISOFLUROPHATE
|
-indirect cholinergic agonist
-irreversibly inhibits cholinesterase |
|
ISOFLUROPHATE
admin, DOA, use |
admin: topical ocular
DOA: 1+ wks use: COAG & strabismus (accommodative esotropia) |
|
MALATHION
|
-indirect cholinergic agonist
-irreversibly inhibits cholinesterase |
|
MALATHION
admin, DOA, use |
admin: topical
DOA: 1+ wks use: pediculosis (lice) |
|
CISAPRIDE
|
-indirect cholinergic agonist
-increases ACh release in enteric & myenteric nervous system -used to increase GI motility |
|
METOCLOPRAMIDE
|
-indirect cholinergic agonist
-increases ACh releasein enteric & myenteric nervous system -used to increase GI motility |
|
SILDENAFIL
|
-NEW cholinergic agonist for erectile dysfunction
DOA: 1-2 hrs. MOA: inhibits breakdown of cGMP by 5-phosphodiesterase-->increased cGMP-->VD metabolism: via cyto P450 (CYP3A4)--> fecal excretion; metabolism inhibited by cimetidine, cisapride, erythromycin, & ketoconazole contraindicated: nitroglycerine pts. (also increase cGMP)-->hypoTN & death |
|
belladonaa alkaloids
list |
atropine, hyoscyamine, scopolamine
tropic acid esters from solanaceous plant in temperate climates PD="fair lady" |
|
ATROPINE
|
-muscarinic antagonist
-Belladonna alkaloid -tropic acid ester -tert. amine |
|
SCOPOLAMINE
|
-muscarinic antagonist
-Belladonna alkaloid -tropic acid ester -tert. amine |
|
ATROPINE & SCOPOLAMINE
uses |
eye: to dilate for eye exam & refraction; treat iritis & cyclitis
heart: treat sinus bradycardia after MI (IV admin); increases AV conduction in AV block pts. GI/GU: to relieve intestinal/bladder spasms & pain CNS: treat Parkinsons pts. Scope: transdermal: prevents motion sickness (MOA: blocks neurotransmission from ear to vomit center in brain stem; DOA: 3 days) other: atropine: reverse anti-AChE overdose |
|
ATROPINE & SCOPOLAMINE
effects |
general: inhibit parasym. --> relax Sm.M, increase HR & conduction, inhibit exocrine gland secretion [inhibit SLUD=salivation, lacrimation, urination, defaction]
eye: PD (iris sph. m relax); cycloplegia (ciliary M. relax); inhibit lacrimal gland heart: increase HR; inhibit Vagal N--> increase conduction rate; **IV admin: 1st slow HR then fast HR as dose increases Rs: BD, inhibit secretions GI/GU: decreases LES tone-->GE reflux; drecrease intestinal motility, inhibit HCl secretion, relax detrusor-->urinary retention CNS: Scopolamine: sedating; Atropine: brief excitatory then long sedatory, high dose=delirium & hallucination others: inhibit sweating-->hyperthermia -->cutaneous VD (flushing) |
|
HYOSCYAMINE
class, structure, uses, admin |
-muscarinic antagonist
-Belladonna alkaloid -levorotatory isomer of racemic atropine (natural form of atropine found in plants) uses: intestinal spasms admin: oral & sublingual |
|
DICYCLOMINE & OXYBUTYNIN
|
-synthetic muscarinic antagonist
-tert. amine -uses: GI hypermotility & spasms & urinary bladder spasms -admin: oral -excretion: renal |
|
FLAVOXATE
|
-synthetic muscarinic antagonist
-uses: relieve bladder spasms |
|
IPRATROPIUM
|
-synthetic muscarinic antagonist
-quat. amine atropine derivative -admin: inhalation -uses: COPD -distribution: poor lung absorption |
|
PIRENZEPINE
|
-synthetic muscarinic antagonist
-M1 selective -uses: reduces vagally stimulated HCl secretion to treat peptic ulcers by inhibiting release of histamine |
|
TOLTERODINE
|
-synthetic muscarinic antagonist
-uses: treats urinary frequency, urgency & incontinence; very selective for bladder (fewer side effects) -DOA: prolonged by erythromycin & ketoconazole -admin: P.O. Bid |
|
TROPICAMIDE
|
-synthetic muscarinic antagonist
-tert. amine -admin: topical ocular -uses: short term PD for eye exam -DOA: 1hr |
|
TRIMETHAPHAN
|
-nicotinic antagonist at ganglion [N(N) receptor]
effect: -symp. ganglia: hypoTN -parasymp. ganglia: dry mouth, blurred vision, urinary retention uses: HTN emergency; causes hypoTN for neurosurgery (bloodless field) |
|
ATRACURIUM
|
-nondepolarizing NM nicotinic antagonist "curariform"
-(+) charged quat. amine -dist: poor gut absorption; no BBB crossing -metabo: rapid via plasma AChE -DOA: 30 min -effect: some histamine release:BrSp, hypoTN, salivary & Br.secretions; low ganglionic blockade **short duration w/ little side effects: DOC |
|
DOXACURIUM
|
-nondepolarizing NM nicotinic antagonist "curariform"
-(+) charged quat. amine -dist: poor gut absorption; no BBB crossing -excretion: urinary & biliary -DOA: 2 hrs -low histamine release |
|
MIVACURIUM
|
-nondepolarizing NM nicotinic antagonist
-DOA: 15 min |
|
PANCURONIUM
|
-nondepolarizing NM nicotinic antagonist
-DOA: 3hrs |
|
TUBOCURARINE
|
-nondepolarizing NM nicotinic antagonist "curariform"
-(+) charged quat. amine -dist: poor gut absorption; no BBB crossing -excretion: renal & biliary -DOA: 1-2 hrs. **high histamine release & ganglionic blockade --> BrSp, hypoTN, excessive salivary & bronchial secretion, tachycardia |
|
VECURONIUM
|
-nondepolarizing NM nicotinic antagonist "curariform"
-(+) charged quat. amine -dist: poor gut absorption; no BBB crossing -metabo: rapid via plasma AChE **short duration w/ little side effects: DOC |
|
Curariform drugs: mechanisms, effects, uses, interactions
|
-competitively blocks ACh at N(M) receptors in SkM.
-stimulate release of histamine & block autonomic glanglia & muscarinic receptors --> BrSp, hypoTN, salivation, and tachycardia -uses: muscle relaxation during surgery; electroconvlusive therapy to prevent injury from invol. muscles; facilitate intubation -potentiated by inhalational anesthetics, AmG, TCN, & Ca channel blockers; & anti-AChE inhibitors (floods synapse with ACh) |
|
SUCCINYLCHOLINE
|
-depolarizing NM nicotinic antagonist
-mechanism: binds to receptor in SkM--> persistant depolarization; 1st: fasciculations (transient contractions), 2nd: sustained muscle paralysis -uses: to produce muscle relaxation during surgery -metabo: ChE (if ChE level too low--> NM paralysis & apnea) |
|
DOBUTAMINE
|
-catecholamine direct adrenergic agonist
|
|
DOPAMINE
|
-catecholamine direct adrenergic agonist
|
|
EPINEPHRINE
|
-catecholamine direct adrenergic agonist
|
|
ISOPROTERENOL
|
-catecholamine direct adrenergic agonist
|
|
NOREPINEPHRINE
|
-catecholamine direct adrenergic agonist
|
|
ALBUTEROL
|
-noncatecholamine direct adrenergic agonist
|
|
APRACLONIDINE
|
-noncatecholamine direct adrenergic agonist
|
|
CLONIDINE
|
-noncatecholamine direct adrenergic agonist
|
|
OXYMETAZOLINE
|
-noncatecholamine direct adrenergic agonist
|
|
PHENYLEPHRINE
|
-noncatecholamine direct adrenergic agonist
|
|
RITODRINE
|
-noncatecholamine direct adrenergic agonist
|
|
TERBUTALINE
|
-noncatecholamine direct adrenergic agonist
|
|
alpha 1 adrenergic receptor
|
increases IP3 & DAG
effect: Sm. M. contraction |
|
alpha 2 adrenergic receptor
|
dcreases cAMP
effect: inhibits NE release; decreases: aqueous humor, insulin mediates: platelet aggregation, CNS |
|
beta 1 adrenergic receptor
|
increases cAMP
effect: increases renin secretion, HR, heart contractility & conduction |
|
beta 2 adrenergic receptor
|
increased cAMP
effect: glycogenolysis, SmM relaxation, K influx to SkM |
|
beta 3 adrenergic receptor
|
increased cAMP
effect: lipolysis |
|
Dopamine 1 receptor
|
increased cAMP
effect: vascular SmM relaxation |
|
Dopamine 2 receptor
|
decreased cAMP, increased K currents, decreased Ca influx
effect: modulates neurotransmission in sympathetic and CNS |
|
imidazoline receptor
|
increased DAG
effect: natriuresis, decrease sympathetic outflow from CNS |
|
DOBUTAMINE
effect, receptor, use |
B1: cardiac stimulation
B2: VD use: cardiogenic shock, acute heart failure, cardiac stimulation during heart surgery |
|
DOPAMINE
receptor, effect, use |
A1/B1: increased BP
B1: cardiac stimulation D1: renal VD use: cardiogenic shock, septic shock, heart failure, & adjunct to fluid administration in hypovolemic shock |
|
EPINEPHRINE
receptor, effect, use |
A1: VC, increased BP
B1: cardiac stimulation B2: BD use: anaphylactic shock, cardiac arrest, ventricular fibrillation, reduction in bleeding during surgery, prolongation of the action of local anesthetics |
|
ISOPROTERENOL
receptor, effect, use |
B1: cardiac stimulation
B2: BD use: asthma, refractory AV block, refractory bradycardia |
|
NOREPINEPHRINE
receptor, effect, use |
A1: VC, increased BP
use: hypotension & shock |
|
ALBUTEROL
receptor, effect, use |
B2: BD
use: asthma |
|
APRACLONIDINE
receptor, effect, use |
A2: decreased aq. humor
use: COAG |
|
CLONIDINE
receptor, effect, use |
A2/I: decreased sympathetic outflow from CNS
use: HTN |
|
OXYMETAZOLINE
receptor, effect, use |
a1: vc
use: nasal & ocular decongestion |
|
PHENYLEPHRINE
receptor, effect, use |
a1: VC, increased BP, mydriasis (PD)
use: nasal decongestion in viral & allergic rhinitis, ocular decongestion in allergic conjunctivitis, PD for eye exam, maintain BP during surgery, treat drug induced & neurogenic shock |
|
RITODRINE
receptor, effect, use |
B2: BC & uterine relaxation
use: asthma & premature labor |
|
TERBUTALINE
receptor, effect, use |
B2: BD & uterine relaxation
use: asthma & premature labor |
|
COCAINE
receptor, effect, use |
indirect: inhibits NE uptake
use: local anesthesia |
|
EPHEDRINE
receptor, effect, use |
A1: VC
use: nasal decongestion in viral & allergic rhinitis |
|
PHENYLPROPANOLAMINE
receptor, effect, use |
A1: VC
use: nasal decongestion in viral & allergic rhinitis |
|
PSEUDOEPHEDRINE
receptor, effect, use |
A1: VC
use: nasal decongestion in viral & allergic rhinitis |
|
PHENOXYBENZAMINE
|
nonselective A-adrenergic blockers
|
|
PHENTOLAMINE
|
nonselective A-adrenergic blockers
|
|
DOXAZOSIN
|
selective A1-adrenergic blockers
|
|
PRAZOSIN
|
selective A1-adrenergic blockers
|
|
TERAZOSIN
|
selective A1-adrenergic blockers
|
|
NADOLOL
|
nonselective B-adrenergic blockers
|
|
PINDOLOL
|
nonselective B-adrenergic blockers
|
|
PROPRANOLOL
|
nonselective B-adrenergic blockers
|
|
TIMOLOL
|
nonselective B-adrenergic blockers
|
|
ACEBUTOLOL
|
selective B1-adrenergic blockers
|
|
ATENOLOL
|
selective B1-adrenergic blockers
|
|
ESMOLOL
|
selective B1-adrenergic blockers
|
|
METOPROLOL
|
selective B1-adrenergic blockers
|
|
CARVEDILOL
|
A & B adrenergic blocker
|
|
LABETALOL
|
A & B adrenergic blocker
|
|
DOXAZOSIN
receptor blocked, effect, use |
A1 (competitive): VD, decreases vascular resistance & BP, relaxes bladder neck & prostate
use: HTN, urinary retention due to genign prostatic hyperplasia |
|
PHENOXYBENZAMINE
receptor blocked, effect, uses |
A1/A2 (noncompetitive): VD, decreases BP, relaxes bladder neck and prostate
uses: HTN episodes from pheochromocytoma, urinary retention due to benign prostatic hyperplasia |
|
PHENTOLAMINE
receptor blocked, effect, uses |
A1/A2 (competitive): VD, decreased BP
uses: HTN episodes due to pheochromocytoma; necrosis & ischemia after injection of A-adrenergic agonists |
|
PRAZOSIN
receptor blocked, effect, uses |
A1 (competitive): VD, decreased BP, relaxes bladder neck and prostate
uses: HTN, urinary retention due to benign prostatic hyperplasia |
|
TERAZOXIN
receptor blocked, effect, uses |
A1 (competitive): VD, decreased BP, relaxes bladder neck and prostate
uses: HTN, urinary retention due to prostatic hyperplasia |
|
ACEBUTOLOL
receptor blocked, effect, uses |
B1 w/ ISA & MSA: decreases HR, CO, AV node conduction, O2 demand; decreases BP
uses: HTN, cardiac arrhythmias |
|
ATENOLOL
receptor blocked, effect, uses |
B1: decreases HR, CO, AV node conduction & O2 demand; decreases BP
uses: HTN, angina pectoris, acute MI |
|
ESMOLOL
receptor blocked, effect, uses |
B1: decreases HR, CO, AV node conduction, & O2 demand; decreases BP
uses: acute supraventricular tachycardia |
|
METOPROLOL
receptor blocked, effect, uses |
B1 w/ MSA: decreases HR, CO, AV node conduction, O2 demand; decreases BP
uses: HTN, angina pectoris, acute MI |
|
NADOLOL
receptor blocked, effect, uses |
B1/B2: decreases HR, CO, AV node conduction, O2 demand, & BP
uses: HTN, angina pectoris, migraine |
|
PINDOLOL
receptor blocked, effect, uses |
B1/B2 w/ ISA & MSA: decreases HR, CO, BP, AV node conduction & O2 demand
uses: HTN |
|
PROPRANOLOL
receptor blocked, effect, uses |
B1/B2 w/ MSA: decreases HR, CO, BP, AV node conduction, O2 demand
uses: HTN, angina petoris, cardiac arrhythmiaz, hypertrophic subaortic stenosis, essential tremor, migraine, acute thyrotoxicosis, acute MI, pheochromocytoma |
|
TIMOLOL
receptor blocked, effect, uses |
B1/B2: decreases HR, CO, BP, AV node conduction , O2 demand, IOP
uses: HTN, acute MI, migraine, COAG |
|
CARVEDILOL
receptor blocked, effect, uses |
A1/B1/B2: VD, decreases HR, BP; increases CO in heart faiulre pts.
uses: HTN, heart failure |
|
LABETALOL
receptor blocked, effect, uses |
A1/B1/B2 W/ MSA: VD, decreases HR & BP
uses: HTN |
|
ester-type local anesthetics
|
benzocaine, chloroprocaine, cocaine, procaine
|
|
amide-type local anesthetics
|
bupivacaine, etidocaine, lidocaine, mepivacaine, prilocaine, ropivacaine
|
|
inhalation general anesthetics
|
nonhalogenated: NO
halogenated: desflurane, enflurane, halothane, isoflurane, sevoflurane |
|
parenteral general anesthetics
|
fentanyl, ketamine, midazolam, propofol, thiopental
|
|
BENZOCAINE
potency, DOA, admin, uses |
low
medium topical: dermal, laryngeal, oral |
|
CHLOROPROCAINE
potency, DOA, admin, uses |
low
short parenteral: epidural, infiltration, nerve block |
|
COCAINE
potency, DOA, admin., uses |
low
medium topical: laryngeal, nasal, Urogenital |
|
PROCAINE
potency, DOA, admin, uses |
low
short parenteral: infiltration, nerve block, spinal |
|
BUPIVACAINE
potency, DOA, admin, uses |
high
medium parenteral: epidural, infiltration, nerve block, spinal |
|
ETIDOCAINE
potency, DOA, admin, uses |
medium
long parenteral: infiltration, nerve block |
|
LIDOCAINE
potency, DOA, admin, uses |
medium
short parenteral: epidural, infiltration, nerve block, spinal topical: dermal, laryngeal, oral |
|
MEPIVACAINE
potency, DOA, admin, uses |
medium
short parenteral: epidural, infiltration, nerve block, spinal |
|
PRILOCAINE
potency, DOA, admin, uses |
medium
short parenteral: infiltration topical: dermal |
|
ROPIVACAINE
potency, DOA, admin, uses |
high
long perenteral: epidural, infiltration, nerve block |
|
AMPHETAMINE
MOA, use |
-indirect adrenergic agonist via increasing NE release
-use: CNS effects |
|
COCAINE
|
-indirect adrenergic agonist
|
|
EPHEDRINE
|
-mixed action adrenergic agonist
|
|
PHENYLPROPANOLAMINE
|
-mixed action adrenergic agonist
|
|
PSEUDOEPHEDRINE
|
-mixed action adrenergic agonist
|
|
Strong opiods-effects
|
cardiac: VD (via histamine release-->red, itchy, hives
eyes: PC (variable with Meperidone) GI/GU: retention (less with meperidone) Endo: incr. Porlactin & ADH; decr. LH Imm: decreased NK cells Resp.: depressed cough: suppressed (except with Merperidone) CNS: analgesic, sedative, eu/dysphoria, addiction pregnancy: prolongs labor (insignificant with Meperidone) |
|
FENTANYL & SUFENTANIL
uses, admin, effects, |
-continuous relief of severe pain & used as an adjunct to general anesthesia (most potent opioid agonsits available)
-patch -less Nausea than Morphine |
|
MEPERIDINE
uses, effects |
-short term treatment of moderate to severe pain (toxic metabolite) & obstetric or postsurgical analgesia
-NO EFFECT ON COUGH REFLEX; variable effect on pupillary size, less GI/GU retention, less prolongation of labor |
|
METHADONE
uses, admin, effect |
-treats opioid addiction
-P.O. -long-acting opioid (pain blocker) |
|
OXYCODONE
admin, uses |
-P.O. we/ nonopioid analgesic (acetaminophen)
-moderate to severe pain |
|
strong opioid agonists
|
Morphine
Methadone Meperidine Oxycodone Fentanyl Sufentanil |
|
Moderate opioid agonists
|
PROPOXYPHENE
CODEINE |
|
other opioid agonists
|
DEXTROMETHORPHAN
DIPHENOXYLATE LOPERAMIDE TRAMADOL |
|
Mixed opioid agonist-antagonists
|
PENTAZOCINE (P.O. also w/ naloxone (antag.) to prevent IV abuse)
BUTORPHANOL (nasal spray also) NALBUPHINE (antagonist at mu) BUPRENORPHINE (antagonist at kappa) ** all parenteral; MOA: parital agonist effect at mu receptor (exc NAL.); agonist at kappa (exept BUP.) uses: pre/post op & OB analgesia; PO & nasal spray for mod.-severe pain side effects: less addiction, GI/GU retention & Rs depression than strong opioids; Does cause anxiety, nightmares, and psychomimetic effects |
|
opioid antagonists
|
NALOXONE
NALTREXONE MOA: competition w/ opioid uses: treats opioid overdose & dependence **Naloxone=short DOA=give multiple doses **Naltrexone=treats alcohol dependence |
|
CODEINE
MOA, admin, effect |
-converted to morphine via cyto P450 CYP2D6; **Pt.s lacking enz=no pain relief w/ codeine
-in combo w/ nonopioid analgesic for mild-moderate pain relief -prevents coughing |
|
PROPOXYPHENE
effect, use, precautions |
-1/2 analgesic effect of codeine
-in combo w/ acetaminophen for mild-moderate pain (somatic & visceral) -prolonged use=build up of toxic metabolite |
|
TRAMADOL
MOA, admin, uses, side effects, cautions |
-strong analgesic
-dual action: + mu & - S-5 and NE reuptake -P.O. for moderate pain & chronic pain syndromes; -minimal cardio & Rs depression -caution: lowers seizure threshold |
|
DEXTROMETHORPHAN
|
=little analgesic activity
-cough suppressant |
|
DIPHENEOXYLATE
|
-little analgesic activity
-treats diarrhea |
|
LOPERAMIDE
|
-little analgesic activity
-treats diarrhea |
|
antitussives
|
morphine, methadone, fentanyl, sufentanil, oxycodone, codeine, dextromethorphan
(little effect: buprenorphine, tramadol, propoxyphene) |
|
ester type local anesthetics
|
BENZOCAINE
CHLOROPROCAINE COCAINE PROCAINE |
|
amide type local anesthetics
|
BUPIVACAINE
ETIDOOCAINE LIDOCAINE MEPIVACAINE PRIOCAINE ROPIVACAINE |
|
inhalation general anesthetics
|
nonhalogenated: NITROUS OXIDE
halogenated: DESFLURANE ENFLURANE HALOTHANE ISOFLURANE SEVOFLURANE **Halogenated: supress Rs fxn & decr. BP in dose-dep. manner |
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parenteral anesthetics
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FENTANYL
KETAMINE MIDAZOLAM PROPOLOL THIOPENTAL |
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local anesthetics drug properties
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only nonionized penetrate neuronal membranes fo reach receptors on internal surface of Na channels; increase does for inflamed & acidotic pts.
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local anesthetics adverse effects
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CNS: simulated (restlessness, tremor, euphoria) followed by inhibition (drowsiness, sedation); OD=seizures followed by coma & Rs failure; CARDIO: hypoTN, cardiac depression; OD=tacyarrhythmia w/ wide QRS; Esters: hypersensitivity; RX interactions: potientiates NM Blockers (worsens MG)
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COCAINE
effect & uses |
effect: VC;
uses: anesthetize inner nose after nasal surgery |
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PROCAINE & CHLOROPROCAINE
(Admin, distribution, metabo, side effects) |
Admin: PE;
Dist: low potency, short DOA; Metabo: converted to PABA; side effects: HSR (hypersens. Rxn) |
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BENZOCAINE
admin & side effect |
admin: topical;
side effects: HSR |
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LIDOCAINE
admin & uses |
admin: topical or PE;
uses: infiltration (subQ), nerve block, epidural, spinal anesthesia; mixed with prilocaine for venipuncture, IV cannulation, or circumcision |
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ETIDOCAINE
DOA & uses |
like Lidocaine but w/ longer DOA;
uses: infiltration & nerve block anesthesia |
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BUPIVACAINE
uses & side effects |
uses: OB anesthesia;
side effects: cardiac depression |
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MEPIVACAINE
uses & side effects |
uses: OB anesthesia;
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ROPIVACAINE
uses |
uses: OB anesthesia
side effects: less cardiac toxicity than Bupivaine |
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PRILOCAINE admin & metabo
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"-Lidocaine congener; admin: topical & infiltration; metabolie buildup causes metHb-emia
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NITROUS OXIDE
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-least potent; strong analgesia
-rapid induction (low bloo:gas partition coeff. -no cardio or Rs depression -causes euphoria ("laughing gas") |
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Halogenated drugs compared
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Halothane Slow induction, most cardio arrhyth., most metabo=HSR & Hepatitis (give infrequently)
Enflurane, Isoflurane Desflurane, Sevoflurane |
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FENTANYL
admin, uses, combinations |
admin: IV or epidural
uses: anesth. & analg for OB, heart & general surgery combo w/ DROPERIDOL=neuroleptanesthesia to maintian pts. ability to answer questions |
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KETAMINE
MOA, admin, effects |
acts like PCP by blocking NMDA receptor for glutamate (less sensory distortion and euphoria)
IV=dissociative anesthesia (incomplete loss of consciousness=analgesia, decr. snes. perception, immobility & amnesia effects: HTN (no Rs effect); delirium, hallucinations, irrational behavior (adults > kids) |
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MIDAZOLAM
DOA, uses, reversal |
-short acting benzodiazepine
-uses: preop. sedation, endoscopy, other diagnostic procedures -reversed by Flumazenil |
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PROPOFOL & THIOPENTAL
MOA, uses, DOA, distribution, effect |
MOA: potentiate GABA;
uses: induce anesthesia; DOA: onset rapid; (unconscious in 20 sec.); lasts 5 min.b/c of fast redistribution from CNS; Thiopental: in fat & muscles; slow elimination=hangover |
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drugs that activate B1
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Cardiac stimulators:
Dobuamine Dopamine Isoproterenol (some epi) |
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drugs that activate A1:
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VC, increased BP, PD, urine retention:
Dopamine Epi Norepi Oxymetazoline Phenylephrine Ephedrine Phenylpropanolamine Pseudoephedrine |
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drugs that activate B2:
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Bronchodilation:
Epi Albuterol Ritodrine (also does uterine relaxation) Terbutaline (also does uterine relaxation) |
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drugs that activate A2:
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Apraclonidine: decreases aqueous humor
Clonidine: decreases sympathetics from CNS |
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drugs that bind Dopamine receptors
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Dopamine: renal VD
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function of MAO & COMT
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reapidly inactivate catecholamines; therefore catecholes must be given Parenterally
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Catecholamine adverse effects
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excessive VC, tissue ischemia, necrosis;
localized ischemia from IV extravasation or epi injected into finger; excessive cardiac stimulation-->arrhythmias glycogenolysis-->hyperglycemia |
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DOC for anaphylactic shock
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Epi=Bronchodilation & increases BP; counteracts histamine released during HSR
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Drugs used to treat HTN caused by vasodilators
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Norepi & Phenylephrine
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drug for cardiac stimulation during heart surgery & short term management of heart failure & cardio shock
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Dobuamine
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drug used to treat refractory bradycardia & AV block
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Isoproterenol
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drugs that acts via decongestion for rhinitis & conjunctivitis (via VC)
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Phenylephrine, Oxymetazoline, Ephedrine, Pseudoephedrine, & Phenylpropanolamine
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drug that causes pupillary dilation without causing cycloplegia
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Phenylephrine
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drug to maintain BP during surgery
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Phenylephrine
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TERBUTALINE
admin, uses |
inhalation asthma
& COPD |
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RITODRINE
admin, uses |
IV
premature labor |
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"ART" drugs adverse effects:(Albuterol, Ritodrine, Terbutaline)
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"TNT": Tachycardia, nervousness, tremor
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list Imidazoline drugs
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OXYMETAZOLINE
APTRCLONIDINE CLONIDINE |
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Imidazoline drug used to treat Chronic HTN
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Clonidine
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CLONIDINE
adverse effects: |
sedative & CNS side effects
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OXYMETAZOLINE
side effects |
CNS & cardiovascular depression
***use w/ caution in kids & elderly |
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AMPHETAMINE
MOA, effects |
increases NE releases;
VC, cardiac stimulation, increased BP, CNS stimulation |
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TYRAMINE
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in foods;
metabolized via MAO; blocking MAO=HTN if such foods are eaten by a pt. On an MOAI; |
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COCAINE
effects |
VC & cardiac stimulation-->elevates BP
in drug abusers: causes ischemia & necrosis of nasal mucosa, HTN & cardiac arrhythmias |
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adrenergic agonist that can act as an appetite suppressant
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phenylpropanolamine
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DOA and admin for noncatecholameins (Ex phenylephrine & albuterol)
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high b/c not destroyed by MAO or COMT; effective P.O.
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PHENOXYBENZAMINE
MOA, DOA, effect |
non-competitive non-specific alpha blocker by covalently binding to receptor
DOA: 4 days effect: decreases BV resistance & BP (VD), urinary bladder neck & prostate relaxation |
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PHENTOLAMINE
MOA, effect, admin, contraindicated |
comptetive non-sepecific apha blocker
effect: VD admin: IV, IM, or subQ contra: chronic HTN Pts (b/c of reflex tachycardia, dizziness, HA, & nasal congestion |
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drug used to manage HTN episodes in pheochromocytoma pts. (note elevated Epi & NE in urine)
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Phenoxybenzamine
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drug used to treat necrosis & ischemia due to extravasation or accidental injection of epi or other vasopressor amine
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Phentolamine
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DOXAZOSIN
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admin: IV
metabo: hepatic DOA: long effect: relax BV muscle (VD), relax prostate & bladder neck Sm.M uses: urinary retention due to BPH; chronic essential (primary) HTN |
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PRAZOSIN
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admin: IV
metabo: hepatic DOA: short effect: relax BV muscle (VD), relax prostate & bladder neck Sm.M uses: urinary retention due to BPH; chronic essential (primary) HTN |
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TERAZOSIN
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admin: IV
metabo: hepatic DOA: long effect: relax BV muscle (VD), relax prostate & bladder neck Sm.M uses: urinary retention due to BPH; chronic essential (primary) HTN |
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list & give adverse effects of selective alpha 1 blockers
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DOXAZOSIN, PRAZOSIN, TERAZOSIN ("AZOSIN" DRUGS) hypoTN, dizziness, fainting, palpitation, edema, first dose syndope (Great effect on BP upon initial admin);
**no tachycardia like non-selective alpha blockers b/c blocking alpha 2 on symph. Neurons prevents feedback inhibition of NE release-->increase activation of cardiac B1 receptors --> tachycardia |
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effect of blocking B1 receptors
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slow, weak pumping heart
deccreased renin secretion decreased aq. Humor |
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effect of blocking B2 receptors
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Bronchoconstriction (in asthmatics)
inhibits epi-stimulated glycogenolysis in liver & slows recovery of blood sugar after a hypoglycemic episode in DM pts. Mask early signs of hypoglycemia (such as tachycardia & sweating) |
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PINDOLOL
effect on B receptors |
partial agonist (intrinsic sympathomimetic) activity (ISA); observed when pt. Is resting & sympathetic tone is low; results in a smaller reduction in HR than other B blockers
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which B-blockers have local anesthetic activity or membrane stabilizing activity?
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Propranolol (& some Pindolol)
blocks Na channels in nerves and heart |
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drug used ONLY to treat HTN (HINT: Beta blocker)
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Pindolol
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PROPRANOLOL
uses, distribution |
HTN, angina, cardiac arrhythmia, hypertrophic subaortic stenosis, essential tremor, migraine, acute thyrotoxicosis, acute MI, pheochromocytoma
high lipid solubility = greater CNS side effects |
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long acting drug (b-blocker) used to treat HTN, angina, and migraine prevention
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Nadolol
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TIMOLOL uses
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P.O.: reduce risk of death in MI pts. & migraine prevention
topcial ocular: COAG |
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drug & admin used to treat acute supraventricular tachycardia occuring during surgery
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Esmolol (selective B1-blocker w/ very short T1/2)
IV |
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B1 blocker admin P.O. to treat HTN & cardiac arrhythmia (also give DOA)
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Acebutolol
DOA: 12 hours b/c metabolite is active |
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B1 blocking side effects
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some bronchoconstriction
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B-blocker with low CNS effects & uses
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Atenolol
HTN, angina, MI |
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METOPROLOL
uses |
HTN, angina, MI
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LABETALOL
MOA, effect, uses |
nonselective B blocker, selective A1 blocker
decreases HR & CO (by blocking B) VD (by blocking A1) uses: HTN treatment |
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CARVEDILOL
MOA, effect, uses |
nonselective B blocker, selective A1 blocker
decreases HR & CO (by blocking B) VD (by blocking A1) uses: HTN treatment & decreases cardiac afterload & increases CO in heart failure pts. |