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Drugs for ANS

Ch. 14

Adrenergic Drugs definition drugs that stimulate the SNS (sympathetic NS) Also known as: adrenergic agonists, sympathomimetics, catecholamines
What are catecholamines neurotransmitters for SNS, mimic response "Flight or fight": endogenous (epi,norepi,dopamine) and Synthetic (dobutamine, phenylephrine)
What are adrenergic receptors throughout body, receptors for SNS neurotransmitters: alpha, beta, dopaminergic receptors (only respond to dopamine)
Adrenergic responses vasoconstriction, CNS stimulation, mydriosis (pupil dilate), dry mouth, incr HR, bronchodilation, bladder fundus relaxes, sphincter contracts
Beta adrenergic receptors B1 - heart B2 - lungs, visceral organs
Beta adrenergic responses smooth muscle relax, glycogenolysis (break down glucagen to glucose), cardiac accel, incr contractility, broncho relax, uterine relax, incr renin secretion, incr BP, vasodilate arterioles to skeletal muscles
Results of cardiac stimulation incr force of contraction (inotropic) incr HR (chronotropic) incr conduction thru AV node (dromotropic)
What do vasoactive sympathomimetics do? pressors/inotropes, support heart during failure or shock, incr BP, epinephrine
How treat eyes? Glaucoma- reduce intraocular pressure, dilation of pupils, alpha adrenergic receptors, epi, dipifefrin Conjunctival congestion
how treat nose? nasal congestion- constrict dilated arterioles, alpha adren. receptors
Cautions for two adrenergics drugs can cause? severe cardiovascular effects such as tachycardia or hypertension
Adrenergic Blockers adrenergic antagonists, sympatholytics, a blockers, b blockers, a/b blockers,
A Blockers effects and indications treat migraines, induce local vasoconstriction for controlling bleeding, htn, BPH
B Blockers indications antiangina (chest pain), cardioprotective, class II antidysrhythmics (get heart back in normal rhythm), antihypertensive, heart failure, migraines
Cholinergic Drugs stimulate Parasympathetic NS think colon, "rest and digest" Neurotransmitter: Ach (acetylcholine)
SLUDGE acronym S-salivation L- lacrimation (tears) U- urinary incontinence D- diarrhea G- gastrointestinal cramps E- emesis (vomit)
Drug effects of Cholinergic drugs incr gi mucus, bladder fundus contract, miosis (pupil constriction), incr sweating/saliva, reduce HR, vasodilation, bronchoconstriction
Drugs for glaucoma Drugs for urinary retention Pilocarpine Bethanechol
Overdose is life threatening, what is remedy Atropine is antidote
Cholinergic Blocking Drugs inhibit Ach actions, anticholinergics, "I can't see, pee, spit, sh_t", antimuscarinic
Drug effects: cardio and CNS small dose: decr HR; lg dose: incr sm: decr muscle rigidity/tremors (parkinson's); lg: drowsy,hallucinate
Drug effects: eye and gastro mydriasis - dilate, decr. accommodation can't poop, decr gastric secretions (can't spit)
Drug effects genitourinary and glandular and resp relaxed detrusor muscle, incr constriction of int. sphincter = retention decr salivation and sweat decr bronchial secretions, dilate airways
anticholinergics are used to treat IBS, incontinence/bladder spasms, decr resp secretions preop, block vagal impulse to heart, relax sphincter iris, tremors/rigid Parkinsonism, SE psychotropic meds
Atropine is an anticholinergic used for heart block, severe bradycardia
Overdose is life threatening and the antidote for atropine overdose is physostigmine and may cause sensitive to light and decr sweating so be at higher risk for heat stroke
Alpha1 receptors excite/stimulate, nasal congestion, hypotension, dilation of pupils for eye examination, GI, GU, arterioles
Alpha2 receptors hypertension (HTN), relax/inhibit norepi, smooth muscles, pancreas, salivary, skin, mucosa
Beta1 receptors cardiac arrest, heart failure, shock, heart brain kidney, lipocytes
Beta2 receptors asthma and premature- labor contractions, smooth muscle of eye, aa, vv, bronchioles, liver, pancrea, GI, GU
Alpha2 Agonists Slow heart rate and cause vasodilatation by working centrally in the brain, can cause retention of NA, so diuretic given with Clonidine: 2nd line: Lowers blood pressure and heart rate/Tx withdrawal symptoms/ADHD
Clonidine (Alpha2 Agonists) ADRs drowsiness, dry mouth, constipation, retention, impotence, nightmars, insominia, hypohtn, brady, rebound htn w withdrawal
Clonidine Clinical Use & Dose Use: lower BP, HR, tx withdrawal sys, ADHD Dose: 0.1mg BID
Alpha2 Agonists Preg Cat. methyldopa- 1st line preg, Cat B, Clonidine Cat. C, breast
Clonidine Alpha2 Agonists Monitor/education Mon: 50% met liver - liver failure, recent MI, depression, coronoary insuff Ed: x BBB/placenta, withdraw slowly
Beta 2 Agonists Bronchodilation is main use of these drugs Albuterol: bronchodilation
Beta 2 Agonists ADRS
Beta 2 Agonists Clinical Use relax bronchioles, albuterol, ephedrine, levalbuterol, pirbuterol, terbutaline/Brethine(asthma) (stops premature labor)
Beta 2 Agonists Monitoring/Education
Adrenergic Antagonists - Alpha/Beta blockers Action: block alpha receptors leading to vasodilatation Tx: HTN, benign prostatic hyperplasia (BPH), Raynaud’s disease, and migraine headaches
Beta blockers Action: antagonize or block the effects of catecholamines Drugs can be “selective” to beta1 receptors or “nonselective” to beta1 receptors Mainly used: HTN and post myocardial infarction (MI)
Alpha Blockers drugs Prazosin (Minipress): Used for HTN Tamulosin (Flomax): Used for BPH, OL stones, retentn doxazosin(cardure),sildosin(rapaflo),prazosin
Alpha Blockers ADRs ortho hypotn, hypotn, impotence
BB - Selective vs nonselective drugs atenolol : b1 selective(cardiosele) propanolol: nonselctive nebivol: ext met(EM) b1 selec, nonselec for poor met(PM)
BB - Selective vs nonselective drugs clinical use Angina HTN Heart failure Post MI antidysrhythmia Migraine prophylaxis Arrhythmias
Cholinergic Agents: AKA: parasympathomimetics, muscarinic agonists Uses decrease intraocular pressure in glaucoma Tx atony of gastrointestinal tract and urinary bladder Dx/Tx myasthenia gravis *Physostigmine* : tx anticholinergic toxicity
Direct-acting cholinergic drugs Prototype: bethanechol (Urecholine): Increases tone of detrusor muscle/ causes bladder contractions/ Incr gastric tone Prototype: pilocarpine (Pilocar)
Indirect-acting cholinergic drugs Cholinesterase inhibitors Prototype: neostigmine bromide (Prostigmin)
Bethanechol (Urecholine) clinical use Neurogenic bladder atony Not used for reflux
Bethanechol ADRs
Bethanechol Monitor/Education
Anticholinergic Drugs AKA: cholinergic blockers, muscarinic antagonists Prototype: atropine Belladonna tincture Trihexyphenidyl (Artane) Oxybutynin Cl (Ditropan) Scopolamine (Hycosine) Benztropine (Cogentin)
Cholinesterase Inhibitors Myasthenia gravis: Neostigmine and pyridostigmine Alzheimer’s disease: Donepezil (Aricept)
Neostigmine and pyridostigmine ADRs
Donepezil (Aricept) ADRs
Cholinergic Blockers Atropine: prototype drug selection: Scopalamine: motion sickness Ipratropium bromide: bronchodilator Benztropine: extrapyramidal symptoms Oxybutin: bladder spasms
Cholinergic Blockers ADRs
Clonidine interactions alcohol, BB, nitrates, prazosin, TCSs, verapamil
Prazosin(minipress) 1-2mg BID, preg C, for HTN, onset 120-130m, pk 1-3h, 92-97% protein binding, 48-68% bioav, half 2-3h, Ecr: 90%bile, 10%urine
Tamsulosin(flomax) 0.1mg 30m b4 meal, CYP 450 met slowly, pk 5d, 94-99%prot bind, >90bioav, half9-15h, Ecr: <10%urine, DRint: cimetadine
Prazosin(minipress) drug int, monitor, education Drint:BB, clonidine, indomethacin Mon: liver, WBC, fluid retn, BP Ed: take same time ea d, 1st dose HS
Atenolol 25-50mg/d, Cat D, 60m onset, 2-4h pk, 6-16 prot bind, 50-60%bioav, 6-9hHL,Excr: 50% unch urine/rest feces
propanolol Adult 40mg BID, child 0.5mg/kg/d BID, onset30m, Pk60-90m, 90%bind, 30%avail, HL3-5h, Excr: <1%unch urine
Atenolol ADRs/drug int/mon/ed adrs: impot/depre/hypo/brady/worsen resp drint: CCB, NSAID, ampicillin, rifampin, salicylates, cipro, dig, antihtn, stim, prazosin, sultonylureas, clonidine mon: glucose (mask hypogly)
Created by: palmerag



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