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Drugs for ANS
Ch. 14
| Question | Answer |
|---|---|
| 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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