EVMS Pharm test 2

Start Studying!

Terms

undefined, object

copy deck

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: 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
PRAZOSIN: 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
TERAZOSIN: 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
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: NITROUS OXIDE
halogenated: DESFLURANE
ENFLURANE
HALOTHANE
ISOFLURANE
SEVOFLURANE

**Halogenated: supress Rs fxn & decr. BP in dose-dep. manner
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
parenteral anesthetics: FENTANYL
KETAMINE
MIDAZOLAM
PROPOLOL
THIOPENTAL
local anesthetics drug properties: only nonionized penetrate neuronal membranes fo reach receptors on internal surface of Na channels; increase does for inflamed & acidotic pts.
local anesthetics adverse effects: 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)
COCAINE effect & uses: effect: VC;
uses: anesthetize inner nose after nasal surgery
PROCAINE & CHLOROPROCAINE (Admin, distribution, metabo, side effects): Admin: PE;
Dist: low potency, short DOA;
Metabo: converted to PABA;
side effects: HSR (hypersens. Rxn)
BENZOCAINE admin & side effect: admin: topical;
side effects: HSR
LIDOCAINE admin & uses: admin: topical or PE;
uses: infiltration (subQ), nerve block, epidural, spinal anesthesia; mixed with prilocaine for venipuncture, IV cannulation, or circumcision
ETIDOCAINE DOA & uses: like Lidocaine but w/ longer DOA;
uses: infiltration & nerve block anesthesia
BUPIVACAINE uses & side effects: uses: OB anesthesia;
side effects: cardiac depression
MEPIVACAINE uses & side effects: uses: OB anesthesia;
ROPIVACAINE uses: uses: OB anesthesia
side effects: less cardiac toxicity than Bupivaine
PRILOCAINE admin & metabo: "-Lidocaine congener; admin: topical & infiltration; metabolie buildup causes metHb-emia
NITROUS OXIDE: -least potent; strong analgesia
-rapid induction (low bloo:gas partition coeff.
-no cardio or Rs depression
-causes euphoria ("laughing gas")
Halogenated drugs compared: Halothane Slow induction, most cardio arrhyth., most metabo=HSR & Hepatitis (give infrequently)
Enflurane, Isoflurane
Desflurane, Sevoflurane
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
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)
MIDAZOLAM DOA, uses, reversal: -short acting benzodiazepine
-uses: preop. sedation, endoscopy, other diagnostic procedures
-reversed by Flumazenil
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
drugs that activate B1: Cardiac stimulators:
Dobuamine
Dopamine
Isoproterenol
(some epi)
drugs that activate A1:: VC, increased BP, PD, urine retention:
Dopamine
Epi
Norepi
Oxymetazoline
Phenylephrine
Ephedrine
Phenylpropanolamine
Pseudoephedrine
drugs that activate B2:: Bronchodilation:
Epi
Albuterol
Ritodrine (also does uterine relaxation)
Terbutaline (also does uterine relaxation)
drugs that activate A2:: Apraclonidine: decreases aqueous humor
Clonidine: decreases sympathetics from CNS
drugs that bind Dopamine receptors: Dopamine: renal VD
function of MAO & COMT: reapidly inactivate catecholamines; therefore catecholes must be given Parenterally
Catecholamine adverse effects: excessive VC, tissue ischemia, necrosis;
localized ischemia from IV extravasation or epi injected into finger;
excessive cardiac stimulation-->arrhythmias
glycogenolysis-->hyperglycemia
DOC for anaphylactic shock: Epi=Bronchodilation & increases BP; counteracts histamine released during HSR
Drugs used to treat HTN caused by vasodilators: Norepi & Phenylephrine
drug for cardiac stimulation during heart surgery & short term management of heart failure & cardio shock: Dobuamine
drug used to treat refractory bradycardia & AV block: Isoproterenol
drugs that acts via decongestion for rhinitis & conjunctivitis (via VC): Phenylephrine, Oxymetazoline, Ephedrine, Pseudoephedrine, & Phenylpropanolamine
drug that causes pupillary dilation without causing cycloplegia: Phenylephrine
drug to maintain BP during surgery: Phenylephrine
TERBUTALINE admin, uses: inhalation asthma
& COPD
RITODRINE admin, uses: IV
premature labor
"ART" drugs adverse effects:(Albuterol, Ritodrine, Terbutaline): "TNT": Tachycardia, nervousness, tremor
list Imidazoline drugs: OXYMETAZOLINE
APTRCLONIDINE
CLONIDINE
Imidazoline drug used to treat Chronic HTN: Clonidine
CLONIDINE adverse effects:: sedative & CNS side effects
OXYMETAZOLINE side effects: CNS & cardiovascular depression
***use w/ caution in kids & elderly
AMPHETAMINE MOA, effects: increases NE releases;
VC, cardiac stimulation, increased BP, CNS stimulation
TYRAMINE: in foods;
metabolized via MAO;
blocking MAO=HTN if such foods are eaten by a pt. On an MOAI;
COCAINE effects: VC & cardiac stimulation-->elevates BP
in drug abusers: causes ischemia & necrosis of nasal mucosa, HTN & cardiac arrhythmias
adrenergic agonist that can act as an appetite suppressant: phenylpropanolamine
DOA and admin for noncatecholameins (Ex phenylephrine & albuterol): high b/c not destroyed by MAO or COMT; effective P.O.
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
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
drug used to manage HTN episodes in pheochromocytoma pts. (note elevated Epi & NE in urine): Phenoxybenzamine
drug used to treat necrosis & ischemia due to extravasation or accidental injection of epi or other vasopressor amine: Phentolamine
list & give adverse effects of selective alpha 1 blockers: 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
effect of blocking B1 receptors: slow, weak pumping heart
deccreased renin secretion
decreased aq. Humor
effect of blocking B2 receptors: 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)
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
which B-blockers have local anesthetic activity or membrane stabilizing activity?: Propranolol (& some Pindolol)
blocks Na channels in nerves and heart
drug used ONLY to treat HTN (HINT: Beta blocker): Pindolol
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
long acting drug (b-blocker) used to treat HTN, angina, and migraine prevention: Nadolol
TIMOLOL uses: P.O.: reduce risk of death in MI pts. & migraine prevention
topcial ocular: COAG
drug & admin used to treat acute supraventricular tachycardia occuring during surgery: Esmolol (selective B1-blocker w/ very short T1/2)

IV
B1 blocker admin P.O. to treat HTN & cardiac arrhythmia (also give DOA): Acebutolol
DOA: 12 hours b/c metabolite is active
B1 blocking side effects: some bronchoconstriction
B-blocker with low CNS effects & uses: Atenolol
HTN, angina, MI
METOPROLOL uses: HTN, angina, MI
LABETALOL MOA, effect, uses: nonselective B blocker, selective A1 blocker
decreases HR & CO (by blocking B)
VD (by blocking A1)
uses: HTN treatment
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.

Start Studying!

Deck Info

Number of cards 232