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Glossary of EVMS Pharm test 2

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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.

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