Ch. 14
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| Adrenergic Drugs definition | drugs that stimulate the SNS (sympathetic NS)
Also known as: adrenergic agonists, sympathomimetics, catecholamines
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| What are catecholamines | neurotransmitters for SNS, mimic response "Flight or fight": endogenous (epi,norepi,dopamine) and Synthetic (dobutamine, phenylephrine)
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| What are adrenergic receptors | throughout body, receptors for SNS neurotransmitters: alpha, beta, dopaminergic receptors (only respond to dopamine)
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| Adrenergic responses | vasoconstriction, CNS stimulation, mydriosis (pupil dilate), dry mouth, incr HR, bronchodilation, bladder fundus relaxes, sphincter contracts
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| Beta adrenergic receptors | B1 - heart
B2 - lungs, visceral organs
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| 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
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| Results of cardiac stimulation | incr force of contraction (inotropic)
incr HR (chronotropic)
incr conduction thru AV node (dromotropic)
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| What do vasoactive sympathomimetics do? | pressors/inotropes, support heart during failure or shock, incr BP, epinephrine
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| How treat eyes? | Glaucoma- reduce intraocular pressure, dilation of pupils, alpha adrenergic receptors, epi, dipifefrin
Conjunctival congestion
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| how treat nose? | nasal congestion- constrict dilated arterioles, alpha adren. receptors
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| Cautions for two adrenergics drugs can cause? | severe cardiovascular effects such as tachycardia or hypertension
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| Adrenergic Blockers | adrenergic antagonists, sympatholytics, a blockers, b blockers, a/b blockers,
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| A Blockers effects and indications | treat migraines, induce local vasoconstriction for controlling bleeding, htn, BPH
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| B Blockers indications | antiangina (chest pain), cardioprotective, class II antidysrhythmics (get heart back in normal rhythm), antihypertensive, heart failure, migraines
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| Cholinergic Drugs | stimulate Parasympathetic NS
think colon, "rest and digest"
Neurotransmitter: Ach (acetylcholine)
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| SLUDGE acronym | S-salivation
L- lacrimation (tears)
U- urinary incontinence
D- diarrhea
G- gastrointestinal cramps
E- emesis (vomit)
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| Drug effects of Cholinergic drugs | incr gi mucus, bladder fundus contract, miosis (pupil constriction), incr sweating/saliva, reduce HR, vasodilation, bronchoconstriction
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| Drugs for glaucoma Drugs for urinary retention | Pilocarpine
Bethanechol
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| Overdose is life threatening, what is remedy | Atropine is antidote
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| Cholinergic Blocking Drugs | inhibit Ach actions, anticholinergics, "I can't see, pee, spit, sh_t", antimuscarinic
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| Drug effects: cardio and CNS | small dose: decr HR; lg dose: incr
sm: decr muscle rigidity/tremors (parkinson's); lg: drowsy,hallucinate
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| Drug effects: eye and gastro | mydriasis - dilate, decr. accommodation
can't poop, decr gastric secretions (can't spit)
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| 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
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| 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
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| Atropine is an anticholinergic used for | heart block, severe bradycardia
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| 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
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| Alpha1 receptors | excite/stimulate, nasal congestion, hypotension, dilation of pupils for eye examination, GI, GU, arterioles
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| Alpha2 receptors | hypertension (HTN), relax/inhibit norepi, smooth muscles, pancreas, salivary, skin, mucosa
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| Beta1 receptors | cardiac arrest, heart failure, shock, heart brain kidney, lipocytes
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| Beta2 receptors | asthma and premature- labor contractions, smooth muscle of eye, aa, vv, bronchioles, liver, pancrea, GI, GU
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| 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
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| Clonidine (Alpha2 Agonists) ADRs | drowsiness, dry mouth, constipation, retention, impotence, nightmars, insominia, hypohtn, brady, rebound htn w withdrawal
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| Clonidine Clinical Use & Dose | Use: lower BP, HR, tx withdrawal sys, ADHD
Dose: 0.1mg BID
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| Alpha2 Agonists Preg Cat. | methyldopa- 1st line preg, Cat B, Clonidine Cat. C, breast
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| Clonidine Alpha2 Agonists Monitor/education | Mon: 50% met liver - liver failure, recent MI, depression, coronoary insuff
Ed: x BBB/placenta, withdraw slowly
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| Beta 2 Agonists | Bronchodilation is main use of these drugs
Albuterol: bronchodilation
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| Beta 2 Agonists ADRS |
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| Beta 2 Agonists Clinical Use | relax bronchioles, albuterol, ephedrine, levalbuterol, pirbuterol, terbutaline/Brethine(asthma) (stops premature labor)
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| Beta 2 Agonists Monitoring/Education |
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| Adrenergic Antagonists - Alpha/Beta blockers | Action: block alpha receptors leading to vasodilatation
Tx: HTN, benign prostatic hyperplasia (BPH), Raynaud’s disease, and migraine headaches
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| 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)
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| Alpha Blockers drugs | Prazosin (Minipress): Used for HTN
Tamulosin (Flomax): Used for BPH, OL stones, retentn
doxazosin(cardure),sildosin(rapaflo),prazosin
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| Alpha Blockers ADRs | ortho hypotn, hypotn, impotence
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| BB - Selective vs nonselective drugs | atenolol : b1 selective(cardiosele)
propanolol: nonselctive
nebivol: ext met(EM) b1 selec, nonselec for poor met(PM)
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| BB - Selective vs nonselective drugs clinical use | Angina
HTN
Heart failure
Post MI antidysrhythmia
Migraine prophylaxis
Arrhythmias
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| 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
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| Direct-acting cholinergic drugs | Prototype: bethanechol (Urecholine): Increases tone of detrusor muscle/ causes bladder contractions/ Incr gastric tone
Prototype: pilocarpine (Pilocar)
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| Indirect-acting cholinergic drugs | Cholinesterase inhibitors
Prototype: neostigmine bromide (Prostigmin)
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| Bethanechol (Urecholine) clinical use | Neurogenic bladder atony
Not used for reflux
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| Bethanechol ADRs |
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| Bethanechol Monitor/Education |
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| Anticholinergic Drugs AKA: cholinergic blockers, muscarinic antagonists | Prototype: atropine
Belladonna tincture
Trihexyphenidyl (Artane)
Oxybutynin Cl (Ditropan)
Scopolamine (Hycosine)
Benztropine (Cogentin)
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| Cholinesterase Inhibitors | Myasthenia gravis: Neostigmine and pyridostigmine
Alzheimer’s disease: Donepezil (Aricept)
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| Neostigmine and pyridostigmine ADRs |
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| Donepezil (Aricept) ADRs |
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| Cholinergic Blockers | Atropine: prototype
drug selection: Scopalamine: motion sickness
Ipratropium bromide: bronchodilator
Benztropine: extrapyramidal symptoms
Oxybutin: bladder spasms
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| Cholinergic Blockers ADRs |
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| Clonidine interactions | alcohol, BB, nitrates, prazosin, TCSs, verapamil
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| 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
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| 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
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| 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
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| 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
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| propanolol | Adult 40mg BID, child 0.5mg/kg/d BID, onset30m, Pk60-90m, 90%bind, 30%avail, HL3-5h, Excr: <1%unch urine
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| 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)
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