Pharmacology

Acetaminophen

Tylenol

Catecholamines

sympathomimetics, short duration of action, don’t cross BBB

non-Catecholamines

adrenergic agonists, longer half-life, do not undergo degredation by MAO / COMT

Category X

strictest classification; fetal abnormalities reported outweigh potential benefits

Cytochrome P-450

microsomal enzymes responsible for aiding in metabolism of drugs

Tests for Renal Function

BUN, Creatinine, Urine Output,

Tests for Liver Function

ALT, AST,

Cholinergic Agonists

[wet] SLUDGE

Salivation, Lacrimation, Urination, Diarrhea, Gastrointestinal cramps, Emesis = symptoms of cholinergic crisis

Atropine

cholingergic antagonist, can reverse cholinergic crisis

Anticholinergic Effects

[dry] can’t pee, see, sh*t, spit

Alpha 1

vascular tissue; stimulation = vasoconstriction, higher BP

Alpha 2

postganglionic synaptic nerve endings; stimulation = inhibits norepinephrine, decreased BP

Beta 1

heart + kidney; stimulation = increased myocardial contractility, higher HR

Beta 2

smooth muscle (lung, GI, uterine); stimulation = relaxes smooth muscle, bronchodilation

Dopaminergic

stimulation = dilation of renal, mesenteric, coronary and cerebral arteries

Norepinephrine Inactivators

inside neuron: MAO (mono-amine oxidase)

outside neuron: COMT (catechol-o-methyltransferase)

Alpha-Adrenergic Receptors

stimulation of smooth muscle = vasoconstriction of blood vessels, male ejaculation, uterine contraction, bladder sphincter constriction, decreased motility (relaxation of GI smooth muscles)

Beta-1 Adrenergic Receptors

stimulation of myocardial muscle (AV + SA node) = positive inotropy, chronotropy, and dromotropy

Bronchodilators

drugs that stimulate beta-2 adrenergic receptors of bronchial smooth muscles, relaxes

Overactive Bladder

treatment = adrenergic agonists relax detrusor muscle during storage phase of bladder fill cycle; increases bladder storage capacity

Opthalmic Indications

adrenergic agonists = temporarily relieves conjunctival congestion + reduces intraocular pressure, dilation of pupils (treatment for open-angle glaucoma)

Adverse Alpha Effects

headaches, restlessness, excitement, insomnia, euphoria, chest pain, vasoconstriction, reflexive bradycardia, palpitations, dysrhythmias, anorexia(lack of appetite), dry mouth, nausea, vomiting, taste changedizz

Adverse Beta Effects

dizziness, nervousness, headache, mild tremors, increased HR, palpitations, BP fluctuations, sweating, nausea, vomiting, cramps

Dobutamine

beta-1 specific vasoactive adrenergic drug structurally similar to dopamine

stimulates beta-1 receptors on myocardium, increased CO with contractility (positive inotropy) → increased SV

Midodrine

proamatine — prodrug, converts into active form desglymidodrine in liver

alpha-1 adrenergic receptor stimulator, constricts arterioles + veins = peripheral vasoconstriction → treats symptomatic orthostatic hypotension

risk of supine hypertension if given within 4 hours of bedtime / after 6 PM

Norepinephrine

levophed — treats hypotension + shock, direct stimulating beta-adrenergic receptors on heart; stimulates alpha-adrenergic receptors = vasoconstriction

no stimulation to beta2 receptors of lungs, administered via IV infusion

Phenylephrine

neo-synephrine — short term raises BP for patients in shock + controls supraventricular tachycardias, vasoconstriction in regional anaesthesia; almost exclusively works on alpha-adrenergic receptors,

topical form = opthalmic uses + nasal decongestant

Sympatholiytic

adrenergic antagonist

Alpha Blocker

treats HTN (in pheochromocytoma), vasodilates arteries + veins; relieves benign prostatic hyperplasia (urinary obstruction)

treated raynaud’s disease, acrocyanosis & frostbite

Orthostatic Hypotension

caused by alpha-blockers, treated w fluids + volume expanders (albumin)

if BP low enough, give vasopressors

Tamsulosin

flomax — alpha blocker treats BPH, used for female patients w urinary retention / kidney stones

causes retrograde ejaculation (contraindication w erectile dysfunction drugs ex sildenafil)

Beta Blocker

“olol” / “alol” suffix — selective / nonselective, competes w (nor)epinephrine = vasoconstriction of blood vessels, lowers BP, slows HR

beta1 = cardioselective, beta2 = smooth muscle of bronchioles + blood vessels

Atenolol

tenormin — cardioselective beta-blocker to treat hypertension + angina, prevents heart attacks in people who’ve had them, also manages thyrotoxicosis

Carvedilol

coreg — nonselective beta-blocker, alpha1-blocker, calcium channel blocker & potential antioxidant

treats heart failure, angina, HTN; slows progression of failure to decrease hospitalization in mild - moderate HF

added to digoxin, furosemide, and ACE inhibitors

Labetalol

normodyne — both alpha-blocker + beta-blocker, treats HTN and hypertensive emergencies

Metropolol

lopresssor — most common beta-1 blocker; oral forms are succinate (extended) & tartrate (immediate); must be monitored if given by IV

Propranolol

inderal — treats tachydysrythmias, subaortic stenosis, migraine headaches and essential tumors; prototypical nonselective beta-1 and beta-2 blocking drug

contraindicated w asthma

Sotalol

betapace — nonselective beta blocker w potent antidysrythmic properties; indicated for management for difficult-to-treat dysrhythmias

Nicotinic Receptor

located in ganglia of PNS + SNS; stimulated by alkaloid nicotine

stimulated by high doses, generally undesireable

Muscarinic Receptor

located post-synaptically in effector organ (smooth muscle, cardiac muscle, glands) of PNS; stimulated by alkaloid muscarine

stimulated by normal doses, generally desireable

Cholinesterase Inhibitors

indirect; block acetylcholinesterase so ACh accumulates

treats MG myasthenia gravis (+ alzheimers), reverses neuromuscular blocking drugs + anticholinergic poisoning

ex physostigmine, pyridostigmine, neostigmine (for neuromuscular blocking)

donezepril, galantamine, rivastigmine (for alzheimer’s)

Miosis

constriction; d/t PNS

Bethanechol

urecholine — treats acute postoperative + postpartum nonobstructive urinary retention / management r/t neurogenic atony of bladder; acts within 60 min of administration

direct acting cholinergic agent, can be enhanced by acetylcholinesterase inhibitors

Donezepril

aricept — treats mild alzheimer’s, works centrally in brain to increase ACh by inhibiting acetylcholinesterase; similar to galantamine + rivastigmine

counteracted by anticholinergics + NSAIDs

Pyridostigmine

mestinon — relieves MG by improving muscle strength (symptomatic treatment)

indirect-acting cholinergic drug increases ACh by inhibiting acetylcholinesterase

Edrophonium

tensilon — indirect-acting cholinergic drug differentiates between cholingergic crisis and MG

diagnoses MG if symptoms improve, cholingergic crisis if symptoms worsen (administer atropine)

Oxybutynin

ditropan — synthetic antimuscarinic drug, manage overactive bladder + antispasmodic for neurogenic bladdder r/t spinal injury / spina bifida; available as transdermal patch

contraindicated w GI + urinary retention or uncontrolled angle-closure glaucoma

Scopolamine

naturally occurring cholinergic blocker, principal belladonna alkaloid; most potent antimuscarinic for motion sickness prevention + postoperative nausea / vomitting

correct ACh / norepinephrine imbalance in vomitting part of brain (patch placed on mastoid)

same contraindications as atropine. Stop if drowsiness, dry mouth or blurred vision (will reverse)

Nonsteroidal Anti-Inflammatory Drugs NSAIDs

inhibition of leukotriene and/or prostaglandin pathway; relieves pain, headache and inflammation by blocking cyclooxygenase COX

contraindiction w PUD + vitK deficiency (risks for bleeding)

Aspirin

ASA, ecotrin, bayer — NSAID that inhibits platelet aggregation, irreversible inhibitor of COX-1 receptors w platelets; reduced formation of thromboxane A2

81 mg ASA = prophylaxis treatment for risk of CAD + stroke after MI

Cyclooxygenase

enzyme that converts arachidonic acid into prostaglandins / products (synthesis of prostaglandins causes pain + inflammation at tissue injury site)

COX-1

protects stomach lining, regulates blood platelets

COX-2

triggers inflammation and pain

Salicylates

ex aspirin, bismuth subsalicylate, methyl salicylate (wintergreen)

toxicity causes increases HR, tinnitus, GI upset, sweating, hyperventilation, hypo/hyperglycemia; risk of Reye’s syndrome in children w viral infections / flu symptoms

Ketorolac

toradol — acetic acid derivative; analgesia + anti-inflammatory properties, comparable to narcotics w no dependence / tolerance

MAX 5 days, can cause renal impairment

Propionic Acid Derivatives

ibuprofin (motrin, advil), naproxen — treats dysmenorrhea, anti-pyretic, rheumatoid/osteo-arthritis, gout, dental pain, musculosketal disorders

Cyclooxygenase-2 Inhibitors

made to have less GI effects, lower incidence of bleeding vs NSAIDs

Celecoxib

celebrex — treats dysmenorrhea, osteo/rheumatoid arthritis, acute pain, ankylosing spondylitis; only COX2 inhibitor on market

contraindiction if sulfa allergy

Enolic Acid Derivatives

piroxicam, nabumetone, meloxicam (molic) — manages mild - moderate pain of osteo / rheumatoid / gouty arthritis

Anti-Gout Drugs

allopurinol, febuxostat, colchicine, probenecid — NSAIDs for acute pain

overproduction of uric acid and/or under excretion of uric acid = hyperuricemia → uric acid crystals deposit in joints / tissues → pain + inflammation

Allopurinol

zyloprim — xanthine oxidase inhibitor, prevents uric acid production; treats hyperuricemia in gout + tumor lysis syndrome

Febuxostat

uloric — manages gout, nonpurine selective xanthine oxidase inhibitor (more selective than allopurinol), higher risk of cardiovascular events

Colchicine

manages gout — recommended for acute attacks, may treat prophylaxis; inhibits metabolism, mobility and chemotaxis of polymorphonuclear leukocytes → decreases inflammatory response of urate deposits

Probenecid

urocosuric, manages hyperuricemia in gout; inhibits uric acid reabsorption in kidneys→ increases uric acid excretion

binds to transporter protein in PCT, reabsorbs uric acid (urine → blood)

Phenobarbital

barbiturate — therapeutic serum level: 10 - 40 mcg/mL

enzyme enducer = increases metabolism of other drugs (should be taken alone), causes sedation

Phenytoin

hydantoin — therapeutic serum level: 10 - 20 mcg/mL

enzyme enducer = increases metabolism of other drugs (should be taken alone)

→teratogenic, risk of extravasation, gingival hyperplasia; contraindicted w bradycardia, need to monitor albumin

Gabapentin

neurontin — chemical analogue of GABA, high risk of mis-use

Levetiracetam

keppra — common in acute care as prophylaxis for head trauma, can cause CNS depression + fatigue

Parkinson’s Disease

imbalance between excitatory ACh and inhibitory dopamine d/t degeneration of dopaminergic neurons

less dopamine → ACh response exceeds it →increased GABA → symptomatic movements

TRAP: tremors, rigidity, akinesia, postural instability

Monoamine Oxidase Inhibitors MAOI

indirect-acting dopaminergic drug — prevents breakdown of ACh enzymes ex norepinephrine, dopamine, seretonin → increases their levels

treats anxiety / depression / parkinson’s

Tyramine

found in cheese, red wine, beer, sausage, pickled foods, yogurt; non-selective MAOI drugs interact negatively

Flumazenil

romazicon — works via antagonistic effects, competes with benzodiazepine for receptor sites

can cause rebound status epilepticus

Alprazolam

xanax — treats GAD, panic disorder, anxiety r/t depression and acute anxiety symptoms

Diazepam

valium — anxiety, alcohol withdrawal, status epilepticus, sedation, muscle spasms

active metabolites can accumulate w/ liver dysfunction → toxicity

Lorazepam

ativan — intermediate acting, best choice of drug for older adults; treats agitation, alcohol withdrawal, status epilepticus

Lithium Carbonate

narrow therapeutic range, anti-manic affect w/ unclear mechanism

therapeutic serum range 0.8 - 1.2 mEq/L, MUST MONITOR + avoid de/overhydration

Amitriptyline

treats insomnia, neuropathic pain (sometimes depression); anti-cholinergic properties (dry)

may cause discolored urine

Duloxetine

cymbalta — SNRI, treats GAD, depresssion (off-label treats neuropathy + fibromyalgia)

can worsen closed-angle glaucoma

Fluoxetine

prozac — treats depression, bulimia, OCD, panic disorder, premenstrual dysphoric disorder

Trazodone

Desyrel — triazolopyridine, SSRI w minimal effect to norepinephrine reuptake

manages depression + insomnia; strong sedative, impairs cognitive function, can cause priapism d/t alpha-adrengergic blockade

Phenothiazines

largest class of anti-psychotic drugs — block dopamine receptors (D-2 + 5-HT2) post-synaptically in basal ganglia and limbic system → decrease dopamine concentration in CNS

risk of NMG neuroleptic malignant syndrome

Extrapyramidal Symptoms

involuntary motor symptoms (pseudoparkinsonism) ex tardive dyskinesia, acute dystonia, akathisia, choreoathetosis

adverse effect of anti-psychotic drugs ex phenothiazines

CYP450 enzyme

enzyme ingrapefruit that is counterindicted to most antipsychotic drugs

Haloperidol

haldol — a butyrophenone; treats acute agitation + long-term psychosis

antidopaminergic effefts / EPS symptoms

Aripiprazole

abilify — quinoline atypical antipsychotic, treats schizophrenia, bipolar, MDD, agitation

pregnancy category C

Risperidone

risperdal — atypical antipsychotic, treats schizophrenia (negative symptoms); high affinity for alpha1 + alpha2 + histamine H1 receptors

Disulfiram

inhibits aldehyde dehydrogenase (enzyme that metabolizes alcohol)

can’t take if any alcohol consumed in past 12 hours (including mouthwash / cough medicine / desserts)

INTERACTS W METRONIDAZOLE

Naltexrone

for abstinence in alcohol; competitive opioid antagonist (high affinity for mu receptors)

before use, ensure that pt isn’t taking drugs that will bind to opioid receptors d/t risk for eliciting withdrawals

Naloxone

narcan — treats acute opioid overdose, short acting opioid-antagonist attat

Methadone

dolophine — changes the way a brain responds to pain; blocks sense of euphoria from opioids + prevents withdrawals / cravings

Buprenorphine

buprenex — antagonist-agonist for detoxification + maintenance therapy

DXM Dextromethorphan

ingredient in OTC antiussives like robitussin delsym; 18+ ID required to prevent juvenile drug abuse

Captopril

capoten — ACE inhibitor w very short half-life (2 hr), requires more frequent dosing

Enalapril

vasotec — ACE inhibitor, prodrug (requires functioning liver)

can improve outcomes after MI, reduce risk of heart failure

ARB Angiotensin 2 Receptor Blockers

suffix “sartan” — anti-hypertensive drugs that blocks angiotensin 2 from receptor sites

black box warning for pregnancy d/t fetal toxicity

Losartan

cozaar — ARB angiotensin 2 receptor blocker w/ 2 HR half life

Hydralazine

apresoline — vasodilator, acts directly on arterial / smooth muscle

Sodium Nitroprusside

nitropress — titrated based on BP, used in hypertensive emergencies in intensive care

not to be used w impaired cerebral infusion

BNP Brain Natriuretic Peptidde

gold standard for heart failure / fluid overload; more sensitive than ANP in diagnosing heart failure

desired value is <100 pg/mL

Lisinopril

prinivil, zestril — ACE inhibitor; treats hypertension, heart failure, MI

pregnancy category C; risk of dry cough, hyperkalemia, renal failure