Nurs 20025 Pharmacology I Drugs

Phenylephrine

alpha 1 agonist, decongestant

Dopamine (drug)

Alpha1 and Beta1 and Beta2 Agonist

Used to treat shock

Stimulates sympathetic response

Norepinephrine (NE)

the neurotransmitter used by the sympathetic division of the autonomic nervous system at the post-ganglionic organ-level (synapse)

Epinephrine drug class

adrenergic agonist

Midodrine

"Middledrine"

A1 agonist-->vasoconstriction

Use = orthostatic hypotension

SE = supine HTN

Albuterol

Beta 2 agonist (inhalant)

bronchodilator

Isoproterenol

Non-Selective beta agonists- also have B1 agonist properties on the heart (tachycardia, arrhythmias and worsening of angina pectoris) that limit their use

Bethanechol

-Direct cholinergic agonist

-Activates bowel and bladder smooth muscle

-Used in postoperative and neurogenic ileus

-Resistant to AChE

Carbachol

-Direct cholinergic agonist

-Carbon copy of acetylcholine

-Constricts pupils and relieves intraocular pressure in glaucoma

Donepezil drug class

cholinesterase inhibitor

Pyridostigmine

Cholinesterase inhibitor: long−acting (8 h) quaternary carbamate; used in myasthenia gravis

Tiotropium (Spiriva)

Inhaled Anticholinergic

-COPD

Ipratropium

COPD, asthma

muscarinic antagonist

Glycopyrrolate use

anticholinergic

Inhibit GI motility

Prevent bradycardia during surgery

Scopolamine

-Muscarinic antagonist

-Motion sickness

Meclizine (Antivert)

antihistamine that treats motion sickness, dizziness and vertigo. Drowsiness and dry mouth.

Propantheline

-Muscarinic receptor antagonist

-Mechanism: selectively antagonize muscarinic receptor

-Clinical applications: hyperreflexic and overactive bladder, urge incontinence

-Common adverse effects: constipation, diarrhea, nausea, dry mouth, application-site erythema, pruritus, urinary retention

-Contraindications: narrow-angle glaucoma, gastric retention, urinary retention

-THIS DRUG IS A NONSPECIFIC MUSCARINIC RECEPTOR ANTAGONIST

-STARTS WITH P

Dicyclomine

Anticholinergic for cramping/irritable bowel

Atropine

-Muscarinic antagonist

-Used in bradycardia and for ophthalmic applications

-Also used as antidote for cholinesterase inhibitor poisoning

-Actions include increase pupil dilation, cycloplegia, decreased airway secretions, decreased acid secretions, decreased gut motility, decreased bladder urgency in cystitis

-Toxicity: increased body temp (due to decreased sweating), rapid pulse, dry mouth, dry and flushed skin, cycloplegia, constipation, disorientation;

-Can cause acute angle-closure glaucoma in elderly (due to mydriasis), urinary retention in men with prostatic hyperplasia, and hyperthermia in infants

-See also homatropine and tropicamide

Neostigmine

cholinesterase inhibitor

Memantine

NMDA receptor antagonist; anti-Alzheimer's agent

Bethanechol Chloride

Cholinergic agonist

*Levedopa/ Carbidopa (Sinemet)

parkinsons ?

Ropinirole

Dopamine Agonist; Anti-Parkinson's Agent

Tolcapone

-Mechanism: blocks conversion of dopamine to DOPAC by inhibiting central COMT

-Use: Parkinson disease therapy

Entacapone

COMT inhibitor: enhances levodopa access to CNS neurons; adjunctive use in Parkinson's disease. Tox: exacerbates levodopa effects. Tolcapone is similar in action and use but may be hepatotoxic.

Atropine Sulfate

Anticholinergic --antidote for opioids

Benztropine Mesylate

-antiparkinson agent

-cogentin

-dry mouth, blurred vision, constipation, nausea, finger numbness

Dicyclomine Hydrochloride

GI Antispasmodic

Bentyl

Oxybutynin

Ditropan, Ditropan XL Urinary Bladder Modifier

Vasopressin (ADH)

raises blood pressure and makes kidneys conserve water

Captopril

ACE inhibitor : used in HTN, diabetic renal disease, and CHF. Tox: hyperkalemia, fetal renal damage, cough ("sore throat")

Enalapril

ACE inhibitor, antihypertensive

Lisinopril

ACE inhibitor, antihypertensive

Ramipril

ACE inhibitor, antihypertensive

Losartan

Angiotensin II Receptor Blocker (ARB), Antihypertensive

Valsartan

Angiotensin II Receptor Blocker (ARB), Antihypertensive

Olmesartan

Angiotensin II Receptor Blocker (ARB), Antihypertensive

Amlodipine

calcium channel blocker, antihypertensive

Diltiazem

calcium channel blocker, antihypertensive

Verapamil

Calcium channel blocker prototype: blocks "L−type" channels; cardiac depressant and vasodilator; used in HTN, angina, and arrhythmias. Tox: AV block, CHF, constipation

Nicardipine

Calcium channel blocker

USES: HTN emergencies, manage HTN

PK: onset 2-10min, duration 40-60min

ADVERSE: reflex tachycardia, hypotension

Nifedipine

Calcium channel blocker prototype: vasoselective (less cardiac depression); used in angina, HTN. Tox: constipation, headache

Doxazosin

Alpha 1 Blocker; Antihypertensive

Prazosin

alpha 1 antagonist

-treatment of hypertension and BPH

-side effect of postural orthostatic hypotension

Terazosin

Alpha 1 Blocker antihypertensive, also used in BPH

Clonidine

alpha 2 agonist

-treatment for hypertension and opioid withdrawal

-side effects of bradycardia and hypotension

Methyldopa

Alpha 2 Agonist

Stimulates alpha 2 adrenergic receptors (centrally acting antihypertensive), reducing sympathetic outflow from vasomotor centers in the brain.

Indications - HTN

Contraindications - Hepatitis or Cirrhosis

Adverse Effects - sedation, headache, black tongue, orthostatic hypotension.

Guanfacine

Intuniv (ADHD), Tenex (HTN)

Atenelol

Tenormin

Beta Blocker

Metoprolol

beta blocker (trade name Lopressor) used in treating hypertension and angina and arrhythmia and acute myocardial infarction

Propanalol

Obstructs a receptor site for norepinephrine in the heart (antagonist) beta blocker

Carvedilol

Beta-Blocker With Alpha-Blocking Activity; Antihypertensive

Labetalol

Normodyne, Trandate

Antihypertensive

Beta blocker

Hydrochlorothiazide (HCTZ)

THIAZIDE DIURETIC

promotes sodium, chloride, and water excretion (diuresis)

TREAT: HTN and peripheral edema

does not treat immediate emergency diuresis

FIRST DRUG OF CHOICE FOR PERIPHERAL EDEMA

spares calcium= hypercalcemia

affect glucose tolerance = hyperglycemia

ONLY USE IN PATIENTS WITH NORMAL RENAL FUNCTION

***monitor for leg cramps, causes hypokalemia

Spironalactone

-Spironalactone is a K sparing diuretic used for Heart failure.

-Side effects = hyperkalemia monitor 3.5 - 5.0 range.

-ACE, ARB, direct renan blockers, potassium = hyperkalemia.

Furosemide

Loop diuretic prototype: blocks Na+/K+/2Cl− transporter; high efficacy; used in acute pulmonary edema, refractory edematous states, hypercalcemia. Tox: ototoxicity, K+ wasting, hypovolemia, increased serum uric acid

Hydralazine

Vasodilator; Antihypertensive

Nitroprusside

Vasodilator (venous and arterial)

Decreases BP and SVR. May increase HR and CO.

Side effects: CNS effect and cyanide poisoning

0.1-10mcg/kg/min

*Quinidine

Lidocaine

Local anesthetic, medium duration amide prototype: highly selective use−dependent Group IB antiarrhythmic; used for nerve block and post MI ischemic ventricular arrhythmias. Tox: CNS excitation

Propranolol

Beta-Blocker, Nonselective; Antihypertensive

Acebutolol

beta 1 antagonist (partial agonist)

Esmolol

beta 1 antagonist

Amiodarone

antiarrhythmic class III

Dofetilide (Tikosyn)

Family: Antiarrhythmic Class III

Mechanism of action: Inhibit K channels

Admin: Oral

Use: atrial arrhythmias

Side Effects: Long QT

Ibutilide

Corvert

Class III (K+ channel blocker) antiarrhthymic

Indicated for conversion to NSR only, not maintenance

Sotalol

Antiarrhythmics

Class III - K+ Channel Antagonist

By blocking K+ channels responsible for phase 3 repolarization, able to prolong action potential duration and increase effective refractory period in both fast- and slow-response tissues, causing QT-interval prolongation.

Actions - Has potent non-selective class II(beta-blocking) activity.

Used to treat life-threatening ventricular arrhythmias. Also used to maintain sinus rhythm in patients with atrial fibrillation and atrial flutter who are currently in sinus rhythm. Due to its pro-arrhythmic effects, not used for asymptomatic arrhythmias.

Adverse - Has lowest rate of long-term or acute adverse effects. Has similar effects to all beta-blockers as well as dizziness, weakness, and fatigue.

Adenosine

-Antiarrhythmic

-Increase K+ out of cells hyperpolarizing the cell and increasing intracellular Ca2+.

-Drug of choice in diagnosing/abolishing supraventricular tachycardia. Very short acting (~ 15 sec). Effects blunted by theophylline and caffeine (both are adenosine receptor antagonists).

Digoxin

Cardiac glycoside prototype: positive inotropic drug for CHF, half−life 40 h; renal excretion; inhibits Na+/K+ ATPase, also a cardiac parasympathomimetic. Tox: calcium overload arrhythmias, GI upset

antiarrythmic

Nitroglycerin

nitrate drug used in the treatment of angina

Isosorbide Dinitrate

Vasodilator; Antianginal Agent

Isosorbide Mononitrate

Imdur

antianginal

nitrate

dizziness

Bisoprolol

Zebeta

Beta Blocker

Ranolazine

Antianginal agent used to treat chronic stable angina. Only added to regimen if patient remains symptomatic despite optimal doses of beta blocker, Ca channel blocker and long-acting nitrate.

Atorvastatin

Lipitor

HMG-CoA reductase inhibitor

Cholestyramine

bile acid sequestrant, antilipemic

Niacin

Vitamin B3

Angiotensin-converting enzyme (ACE) inhibitors

lower blood pressure by inhibiting the conversion of angiotensin I (an inactive enzyme) to angiotensin II (a potent vasoconstrictor)

Morphine

Opioid analgesic prototype: strong mu receptor agonist. Poor oral bioavailability. Effects include analgesia, constipation, emesis, sedation, respiratory depression, miosis, and urinary retention. Tolerance may be marked; high potential for psychologic and physical dependence. Additive effects with other CNS depressants

Adenosine Diphosphate (ADP)

low-energy molecule that can be converted to ATP

Glycoprotein (GP) IIb/IIIa receptor antagonists

Most effective antiplatelet drugs

"Super aspirins"

Reversible blockade of platelet GP IIb/IIIa receptors

Dobutamine

beta 1 agonist

-inotropic agent, inc. contractility and CO, does NOT inc HR.

-used in acute management of heart failure.

-short 1/2 life due to COMT

**incompatible with bicarb

Phentolamine

-Nonselective α-blocker

-Give to patients on MAO inhibitors who eat tyramine containing foods

-Toxicity: orthostatic hypotension, reflex tachycardia

Milrinone

phosphodiesterase inhibitor, causes increased contractility and vasodilation: "inodilator". Will increase CO and decrease preload and afterload (volume neutral to volume up, prior)

0.375-0.75 mcg/kg/min

may cause arrhythmias and hypotension

therapeutic uses: cardiogenic shock

Nesiritide

Synthetic hBNP. Binds guanylate cyclase receptor-->increased cGMP-->smooth muscle relaxation/dilation-->reduced preload and afterload

Use = rarely used for acute decompensated HF (doesn't help mortality)

SE = hypotension

vasodilator

Sacubitril/Valsartan

Entresto

Neprilysin inhibitor/ARB

Ivabradine

Cardio

MOA: selective inhibition of funny sodium channels, prolonging slow depolarization phase (phase 4); decreases SA node firing; negative chronotropic effect without inotropy; reduces cardiac O2 requirements

Use: chronic stable angina in patients who cannot take beta blockers; chronic HF with reduced ejection fraction

Tox: luminous phenomena/visual brightness, hypertension, bradycardia

Losartan Potassium

Antihypertensive - Angiotensin II Receptor Blocker (ARB)

*Propranalol Hydrochloride

Heparin

Anticoagulant

Enoxeparin (Lovenox)

anticoagulant

Warfarin (Coumadin)

Anticoagulant, Vitamin K Antagonist

Fondaparinux (Arixtra)

Anticoagulant.

Selective inhibitor of factor Xa.

Approved for-

- preventing deep vein thrombosis (DVT) following surgery.

- acute PE/DVT (in conjunction with warfarin).

Administer SubQ. Administered using a fixed dosage, does not require laboratory monitoring.

Cautious use with renal impairment.

Dabigatran (Pradaxa)

Anticoagulant, Direct Thrombin Inhibitor

Rivaroxaban (Xarelto)

Anticoagulant - Direct Factor Xa Inhibitor

Apixaban (Eliquis)

Anticoagulant, Factor Xa Inhibitor

Clopidogrel (Plavix)

antiplatelet agent; tell pt. to avoid injury

Aspirin (ASA)

Non-opioid

non-steroidal

anti-inflammatory

antipyretic

Blood thinner

Aspirin = binds to Cox 1/Cox 2 (stops platelet aggregation, gi upset, tinnitus, HA, sweating)

Abciximab

antiplatelet; glycoprotein IIb/IIIa Inhibitor