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Pharmacology > High Yield Final > Flashcards

High Yield Final Flashcards

1
Q

-gliptin

A
  • DDP-4 inhibitors
  • block degradation of incretins
  • combine with metformin, SU, TZD
  • mod ↓ post-prandial glucose, mild ↓ fasting glucose
  • weight neutral
  • renal elimination
  • well tolerated
  • ↑ risk hypoglycemia with SU.
  • not as strong as exenatide/liraglutide
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2
Q

Abciximab

A
  • anticoagulation drug, platelet inhibitor.
  • blocks GpIIb/IIIa receptor ⇒ rapid reperfusion
  • give IV, long lasting.
  • inhibits fibrinogen-dependent aggregation of activated platelets.
  • use: clot prevention during PCI and prevent restenosis after PCI
  • toxicity: bleeding, 2% thrombocytopenia
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3
Q

Acarbose

A
  • alpha-glucosidase inhibitor.
  • take before meals.
  • inhibits breakdown of complex starches, oligosaccharides, disaccharides
  • delays glucose absorption in GI.
  • delayed glucose delivery to blood = insulin-sparing.
  • side effects: flatulence, diarrhea, abd pain. ↑ risk hypoglycemia with SU.
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4
Q

ACEI

A
  • inhibits ACE that converts angI to angII.
  • minimizes vascular injury, ↓ HTN vascular injury/end organ damage.
  • inhibits kininase ⇒ ↑ bradykinin ⇒ vasodilation, ↓ BP, promotes excretion of Na and water
  • use: HTN, DM, CHF, cerebrovascular disease, renal disease
    • in combo with diuretics, beta blockers, CCB
  • side effects: dry cough, angioedema (in larynx life threatening), ↓ GFR in pt with renal stenosis, fetal nephrotoxicity
  • don’t use: renal artery stenosis, pregnancy
    • switch to -sartan
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4
Q

Acetaminophen

A
  • aka Tylenol
  • analgesic and antipyretic.
  • metabolized in liver: conjugated with glucuronic acid (60%) or sulfuric acid (30%).
  • 1% via CYP450 ⇒ toxic metabolite (benzoquinopomine). glutathione makes it safe.
  • overdose and alcoholics ⇒ ↑ toxic metabolites ⇒ hepatic necrosis.
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5
Q

Acetazolamide

A
  • carbonic anhydrase inhibitor
  • rapid onset (30 min)
  • excreted by tubular S2 segment but acts on S1 segment.
  • inhibits 85% of proximal tubular HCO3- reabsportion
  • inhibits 45% whole kidney HCO3- reabsorption
  • inhibits NHE3 on lumenal side of proximal convoluted tubule ⇒ ↓ Na inside cell ⇒ nonfunctional Na K ATPase on interstitial side. (prevents production of H+ needed for this antiport)
  • also affects Na HCO3- symport on interstitial side from ↓ Na inside cell ⇒ ↓ HCO3- brought to blood.
  • ⇒ ↑ HCO3- excretion, ↑ urinary pH, ↑ urine volume, ↑ Na excretion, ↑ urine K+, ↑ luminal negativity (promotes K excretion)
  • uses: glaucoma - ↓ ocular pressure
    • altitutde sickness prophylaxis - ↓ CSF pH
    • short-term diuretic for edema in CHF - potentiates distally-acting agents, corrects metabolic alkalosis
    • antiepileptic in catamenial epilepsy
    • corrects metabolic alkalosis
    • alkalinates urine - ↑ solubility of uric acid and cystein, ↑ aspirin excretion, ↑ urinary phosphate excretion
  • side effects: hyperchloremic metabolic acidosis, renal stone formation, hyperkalemia
  • contraindications: in K+ depletion, pts with hepatic cirrhosis (may ↑ excretion NH4+ ⇒ hepatic encephalopathy)
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6
Q

Adalimumab

A
  • aka Humira
  • give subQ
  • recombinant human IgG1 monoclonal Ab for TNFalpha.
  • prevents binding of TNF to TNFR1 and TNFR2.
  • can fix complement and bind to Fc receptor.
  • ⇒ apoptosis of monocytes/macrophages and T cells.
  • use: Crohn’s disease, RA, juvenile chronic arthritis, ankylosing spondylitis, psoriasis, psoriatic arthritis, uveitis, IBD.
  • side effects: bacterial infections, TB, opportunistic infections (histo or coccidiomycosis).
  • careful when using with demyelinating disease and SLE.
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7
Q

ADH

A
  • released from posterior pituitary gland when have ↑ plasma osmolality, ↓ BP
    • influenced more by osmolality than BP
  • ⇒ ↑ water reabsorption in collecting duct via V2 receptor stimulation
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8
Q

Albuterol

A
  • short acting beta-2 agonist
  • onset in minutes
  • lasts 4-6 hrs
  • ⇒ down regulation of beta receptors long term.
  • ⇒ vasodilation (bronchodilation)
  • use: asthma, COPD
  • side effects: tachycardia, HTN, tremor, hypokalemia
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8
Q

Alendolate

A
  • bisphosphonate. oral.
  • inhibits FPPS ⇒ ↓ cholesterol, ↓ osteoclast survival.
  • poorly absorbed.
  • ⇒ ↓ risk spine and hip fractures.
  • take before meals
  • use: osteoporosis.
  • side effects: GI irritation, osteonecrosis.
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9
Q

Allopurinol

A
  • competitive inhibitor of Xanthine oxidase
  • ⇒ ↓ synthesis uric acid
  • ↑ alloxanthine ⇒ ↑ solubility and stimulate excretion.
  • use: gout
  • side effects: GI irritation and diarrhea
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10
Q

Alpha-Methyldopa

A
  • alpha-2 agonist
  • safe for HTN in pregnancy
  • use: HTN
  • side effect: hemolytic anemia
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11
Q

Alprazolam

A
  • benzodiazepine with triazole group
  • rapid acting, rapid oral absorption
  • metabolite: alpha-hydroxy metabolites ⇒ liver ⇒ urinary excretion
  • use: relief of anxiety, insomnia, sedation and amnesia before procedures, epilepsy and seizure states, muscle relaxation in neuromuscular disorders, ethanol/sedative-hypnotic withdrawal.
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12
Q

Alteplase

A
  • instead of streptokinase, disolves clots.
  • plasminogen activator.
  • binds Kringle domain, targets plasminogen, digests fibrin
  • given IV, t1/2 = 10-30min, infused slowly
  • use: acute MI (within 6 hr onset STEMI), multiple PE, central DVT, acute thrombotic stroke (within 3hr)
  • don’t use with history of cerebral hemorrhage or recent head injury
  • pt with chronic HTN ⇒ ↑ risk hemorrhagic stroke
  • toxicity: hemorrhage, cerebral ⇒ death
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13
Q

Amantidine

A
  • enhances DA release
  • short-lived effects (wks to months)
  • use: add on for Parkinson’s Disease
  • side effects: CNS effects, peripheral edema, skin discoloration from vasodilation, toxic psychosis, convulsions from overdose.
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13
Q

Amiloride

A
  • K+ sparing Diuretic
  • blocks ENaC in principal cell ⇒ blocks effects of aldosterone
  • promotes acidosis, spares (H+), makes less negative lumen for K+ sparing.
  • uses; Liddle’s syndrome (HTN, ↓ renin, metabolic alkalosis, hypokalemia, normal aldosterone), Lithium induced nephrogenic diabetes insipidus, with thiazides for HTN and edema.
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14
Q

Amiodarone

A
  • impairs T4 → T3 conversion
  • inhibits deiodinase
  • ↑ Na conductance ⇒ slow conductance.
  • K channel blockade, beta blocking, Ca channel blocking
  • prevents re-entry from prolonged refractory period
  • t1/2 = 20 days.
  • widened QT interval.
  • use: prevent PVC, supraventricular and ventricular arrhythmias
  • toxicity: ↓ cardiac contractility, bradycardia, AV block, corneal microdeposits, peripheral neuropathies, pulmonary fibrosis** **
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15
Q

Amitriptyline

A
  • tertiary amine TCA.
  • metabolite = nortriptyline
  • blocks NE and 5-HT
  • use: depression, chronic neuropathic pain syndromes, fibromyalgia, stress incontinence.
  • side effects: dry mouth, blurred vision, ↑ body temp, cognitive impairment, constipation, urinary retention, ↓ seizure threshold, cardiotoxicity, weight gain, orthostatic hypotension, sedation.
  • overdose: agitation, delirium, seizure, coma, fatal cardiac arrhythmias
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16
Q

Amlodipine

A
  • aka Norvasc
  • DHP CCB.
  • blocks entry of Ca into cell ⇒ ↓ Ca induced Ca release.
  • gradual lowering of BP, absorbed slowly, long t1/2
  • synergistic with diuretics
  • take 1x aday. good oral bioavailability
  • ⇒ ↓ stiffness of large arteries, vasodilation, mild diuretic effect.
  • ⇒ ↑ NO release from endothelium ⇒ restore endothelial function and support vasodilation in pts with HTN.
  • block voltage Ca channels ⇒ ↓ cystolic Ca in smooth muscle and ↓ peripheral vascular resistance.
  • use: angina, in old ppl.
  • side effects: peripheral edema, hypotension, tachycardia, palpitations, flushing, headaches, dizziness, nausea
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17
Q

Amphetamine

A
  • ⇒ ↑ DA and ↑ 5HT
  • can cross BBB
  • use: narcolepsy and ADHD
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17
Q

Amphetamine/Metamphetamine

A
  • induce release of NE and DA in CNS.
  • use: ADHD, narcolepsy
  • side effects: chronic abuse at high doses ⇒ paranoid psychosis after 2-3 wks.
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18
Q

AngII Blockers

A
  • target AT1 and AT2 receptors
  • ⇒ ↓ BP thru AT1 receptor blocking
  • use: monotherapy in essential HTN, with diuretics (synergistic)
  • ⇒ ↓ morbidity/mortality in pt with HTN with heart failure, diabetes, and/or end stage renal disease
  • ⇒ ↓ incidence stroke and ↓ clinical features heart failure
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19
Q

ARB

A
  • angiotensin-renin blockers
  • block deleterious effects of AT1 receptors (vasoconstriction and antinaturesis), leaves AT2 effects intact
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20
Q

Aripiprazole

A
  • high potency atypical antipsychotic.
  • blocks 40-60% D2, and 70-90% 5-HT2A.
  • acute = tranquilizer
  • chronic = antipsychotic after a few wks.
  • good for positive symptoms, a little for negative.
  • no weight gain! but less effective.
  • use: schizophrenia, depression, psychosis with manic-depressive/schizoaffective disorders or depression.
  • side effects: sedation, akathisia.
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21
Q

Aspart

A
  • rapid acting insulin
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22
Q

Aspirin

A
  • irreversibly inhibits COX by acetylation
  • affects platelets.
  • 1st pass effect
  • ⇒ analgesic, antipyretic, anti-inflammatory
  • blocks platelet aggregation, ↓ risk colon cancer (PGE2)
  • use: prevent MI and unstable angina, ↓ thrombosis.
  • side effects: GI ulcers, hemorrhage, renal toxicity.
  • overdose: moderate = ↓ PaCO2, ↓ PaHCO3- ⇒ normal pH.
    • severe = inhibits respiratory center ⇒ normal CO2, ↓ HCO3- ⇒ metabolic acidosis ⇒ cardio collapse
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24
Q

Atenolol

A
  • beta-1 antagonist beta-1 >>> beta-2
  • at high doses blocks beta-2
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24
Q

Atorvastatin

A
  • aka Lipitor
  • statin, potent
  • 10mg ⇒ ↓ LDL (35%). 20mg ⇒ 45%, 40mg ↑ toxicity
  • works thru CYP3A4
    • inhibited by grapefruit, erythromycin, ketoconazole
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25
Q

Atracurium

A
  • competitive NMJ blocking agent
  • large and bulkly
  • inhibits amplitude of endplate potentials so propagated action potentials can’t develop
  • ++ histamine release
  • duration: 30-40 mins
  • elimination: spontaneous hydrolysis in plasma = Hofman elimination rxn.
  • use: muscle relaxant, anesthetic.
  • side effects: metabolite = Laudanoside is a CNS stimulator.
  • reversed by ACHEI and ↑ extracellular K+
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26
Q

Atropine

A
  • anticholinergic agent, short acting alkaloid
  • most potent muscarinic antagonist
  • inhibits M1, M2, M3.
  • low dose ⇒ ↓ salivation, ↓ micturition speed
  • high dose ⇒ ↓ salivation, ↓ micturition speed, ↑ HR, ↓ accomodation
  • use: mydriasis, AChEI poisoning
  • lots of side effects: tachycardia, pupillary dilation, urinary retention.
  • interferes with mucociliary clearance.
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27
Q

Azathiprine

A
  • anti-metabolite, looks like purine.
  • blocks DNA synthesis ⇒ blocks proliferating T cells
  • use: immunosuppressive therapy
  • side effect: bone marrow suppression/toxicity.
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28
Q

Beclomethasone

A
  • inhaled corticosteroid
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29
Q

Benztropine

A
  • antimuscarinic, quarternary amine
  • improves tremor and rigidity, little effect on bradykinesia.
  • use: add on for Parkinson’s Disease, COPD
  • side effects: sedation, dry mouth, etc. (anti-muscarinic effects)
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31
Q

Beta Blockers arrhythmias

A
  • slow phase 4 diastolic depolarization (↓ SA node and AV node conduction)
  • prolongs refractory period ⇒ widened QT interval
  • widened refractory period of AV node ⇒ parasympathetic predominance by Ca current
  • accentuates effects of ACh ⇒ hyperpolarization from ↓ Ca.
  • must wean off or may induce tachycardia from upregulated beta receptors.
  • use: ventricular arrhythmias and supraventricular arrhytmias.
  • toxicity: ↓ cardiac contractility, bradycardia, AV block, hypoglycemia, risk of bronchospasm
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31
Q

Beta Blockers

A
  • ⇒ ↓ HR, ↓ periods of ischemia, ↓ mortality in post-MI pts, ↓ cardiac contractility, ↑ LV EDV and P, ↑ wall tension, may ↓ coronary blood flow
  • ↑ diastolic perfusion time, ↑ collateral blood flow ⇒ ↓ CO
  • use: effort-induce angina, angiotensin dependent HTN
  • don’t use: asthma, COPD, severe decompensated heart failure, heart block
  • can interefere with expression of hypoglycemia, cause overdose of insulin
  • with diuretics ⇒ 100% anti-HTN response in essential HTN.
  • cardioprotective for fatal arrhythmias in pts after recent MI.
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32
Q

Betaxolol

A
  • beta-1 >>> beta-2 antagonist
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33
Q

Bethanechol

A
  • direct acting
  • good muscarinic, no nicotinic activity
  • not susceptible to AChE.
  • oral and subQ routes
  • use: post-op/neurologic ileus and urinary retention (boggy bladder)
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33
Q

Brimonide

A
  • alpha-2 agonist
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35
Q

Bromocriptine

A
  • ergot DA receptor agonist
  • inhibits prolactin release
  • less motor recovery and more side effects than L-DOPA.
  • ↓ risk dyskinesias.
  • need careful dosing titration to avoid hypotension.
  • use: Parkinson’s Disease, prolactinomas, infertility and galactorrhea associated with hyperprolactinemia, acromegaly
  • side effects: nausea, vomiting, psychiatric rxns, postural hypotension
  • dose related effects eventually outweight therapeutic effects.
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36
Q

Bupivacaine

A
  • amide local anesthetic
  • metabolized by microsomal hydrolase
  • blocks Na channels from inside axoplasm
  • toxicity: CNS = depress inhibitory neurons ⇒ restlessness, tremor, convulsions.
    • cardio = vasodilation, hypotension, ↓ excitability of cardiac muscle, ↓ conduction velocity, ↓ force of contraction.
  • very little separation btw CNS and cardio side effects.
  • death by respiratory failure.
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37
Q

Buspirone

A
  • 5-HT1A partial agonist ⇒ anxiolytic
  • no hypnotic, anticonvulsant, or muscle relaxant effects.
  • takes 1-2 wks to work
  • no rebound anxiety or withdrawal symptoms
  • nonsedating, less psychomotor impairment, doesn’t impair driving.
  • minimal abuse potential
  • use: generalized anxiety disorder (GAD)
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38
Q

Butorphanol

A
  • opioid analgesic, mixed agonist-antagonist.
  • analgesia from agonist effects on kappa receptors.
  • mu antagonism causes withdrawal in those addicted to strong opioid agonists.
  • use: mild to mod pain, MI, acute dyspnea from heart failure, analgesia, anesthesia
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39
Q

Ca Channel Blockers (CCB)

A
  • use: supraventricular tachycardia
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40
Q

Carbachol

A
  • direct acting agonist
  • good muscarinic and nicotinic activity
  • not susceptible to AChE
  • use: glaucoma
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40
Q

Captropril

A
  • alkyl ACEI.
  • short acting, given 2-3 times per day
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42
Q

Carbidopa

A
  • DOPA-decarboxylase inhibitor.
  • does not penetrate CNS.
  • prevents L-DOPA conversion to DA in periphery.
  • ↑ L-DOPA potency and ↓ nausea, vomiting, and adverse effects from peripheral generation of DA.
  • use: Parkinson’s Disease
  • side effects: ↑ risk dyskinesias, GI adverse effects, postural hypotension, depression, hallucinations, anxiety, agitation.
  • 80% develop dyskinesia with long term use.
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42
Q

Carbamazepine

A
  • prolongs inactivated Na channel.
  • induces CYP3A4 liver enzymes and has autoinduction of metabolism.
  • drug of choice for pt with depression and epilepsy.
  • use: partial seizures, complex partial seizures, tonic-clonic seizures, trigeminal neuralgia, depression, acute manic episodes and prophylaxis.
  • side effects: CNS depression, dilutional hyponatremia (intensifies ADH effects), Steven Johnson’s Syndrome (dermatitis), spina bifida (teratogenic), aplastic anemia, agranulocytosis, sedation, osteomalacia
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44
Q

Carteolol

A
  • beta-1 = beta-2 antagonist
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45
Q

Carvedilol

A
  • beta-1 beta-2 alpha-1 antagonist.
  • O2 radical scavenger.
  • anti-mitogenic ⇒ ↓ renin release, ↓ HR, ↓ myocardial O2 consumption, ↓ downregulation of beta receptors
  • prevents fibrotic changes in ventricl walls, chambers of heart, and vasculature
  • use: short term in HTN crisis
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45
Q

CCB

A
  • DHP or non-DHP
  • can be 1st line for HTN but most in combo with diuretics or aldosterone blockers.
  • can use with ACEI or angII receptor antagonists.
  • ⇒ ↓ systolic BP, ↓ stiffness in larger arteries, vasodilation, mild diuretic effect
  • not as effective at ↓ end organ damage in pt with CHF and end stage renal failure
  • DHP lack cardio-inhibitory actions of non-DHP
  • use in elderly
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46
Q

CCB arrhythmias

A
  • ⇒** ↓ SA node rate and ↓ AV node conduction velocity, ↑ AV node refractory period**.
  • can ⇒ PVC by causing hypotension and stimulating sympathetic outflow
  • not useful for ventricular arrhythmias except abnormal automaticity
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47
Q

Celecoxib

A
  • COX2 inhibitor
  • 30x potent COX2 than COX1 inhibitor.
  • used with aspirin ⇒ ↓ risk thrombosis.
  • does not affect platelet functions or gastric acid secretion.
  • use: RA, osteoarthritis.
  • side effects: ↑ cardiothrombotic events, renal toxicity.
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48
Q

Cervistatin

A
  • statin.
  • too toxic, not on market
  • 200x Fluvastatin
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49
Q

Chlordiazepoxide

A
  • benzodiazepine, halogen group
  • slow acting
  • metabolite = desmethylchlordiazepoxide ⇒ demoxepam ⇒ desmethyldiazepam ⇒ oxazepam ⇒ liver ⇒ urinary excretion
  • use: relief of anxiety, insomnia, sedation and amnesia before procedures, epilepsy and seizure states, muscle relaxation in neuromuscular disorders, ethanol/sedative-hypnotic withdrawal.
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50
Q

Chlorpromazine

A
  • low potency typical antipsychotic.
  • blocks D2 at therapeutic doses.
  • also blocks M1, H1, and alpha-1.
  • takes a few weeks to take effect
  • helps with positive symptoms.
  • use: schizophrenia
  • side effects: block M1 ⇒ increased body temperature, cognitive impairment, constipation, urinary retention, closed-angle glaucoma, decreased seizure threshold, and cardiotoxicity (QT prolongation)
    • block H1 ⇒ weight gain and sedation, ↑ risk type 2 diabetes.
    • block alpha-1 ⇒orthostatic hypotension
    • block D2 ⇒ ↑ prolactin ⇒ galactorrhea, amenorrhea, infertility
    • tardive dyskinesia, parkinsonism.
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51
Q

Cholestyramine

A
  • Bile acid seuestrant
  • binds BA in gut, excreted in feces
  • liver converts more cholesterol to BA ⇒ ↓ cholesterol ⇒ ↑ LDLR and ↓ metabolism of LDLR
  • interferes with absorption of fat-soluble vitamins (A, D, E, K), digitalis, chlorothiazide
  • stagger giving these
  • side effects: staetorrhea, constipation, bloating
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52
Q

Cimetidine

A
  • CYP inhibitor
  • use: stomach ulcer
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52
Q

Cilostazol

A
  • PDE-3 inhibitor ⇒ ↑ cAMP, vasodilation, inhibits platelet function.
  • use: intermittent claudication
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53
Q

Clofibrate

A
  • fibric acid derivative
  • ⇒ ↓ triglyceride levels in blood, ↑ activity of LPL (TG lipase)
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53
Q

Citalopram

A
  • SSRI.
  • selective 5-HT reuptake inhibitor.
  • minimal sedation or autonomic effects.
  • NO WEIGHT GAIN, NO DRUG INTERACTIONS
  • use: depression (1st line), GAD, OCD, phobias, bulimia, pre-menstrual dysphoric disorder, perimenopausal symptoms.
  • side effects: GI discomfort, sexual dysfunction, insomnia, tremor, acute anxiety.
  • discontinuation syndrome if stop suddenly = jittery, anxious, restless.
  • little chance of overdose.
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54
Q

Clomipramine

A
  • tertiary amine TCA.
  • selective 5-HT reuptake inhibitor.
  • use: OCD, depression, chronic neuropathic pain syndromes, fibromyalgia, stress incontinence.
  • side effects: dry mouth, blurred vision, ↑ body temp, cognitive impairment, constipation, urinary retention, ↓ seizure threshold, cardiotoxicity, weight gain, orthostatic hypotension, sedation.
  • overdose: agitation, delirium, seizure, coma, fatal cardiac arrhythmias
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55
Q

Clonidine

A
  • alpha-2 agonist
  • ⇒ ↓ synaptic NE
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56
Q

Clopidogrel

A
  • aka Plavix.
  • DHP platelet inhibitor.
  • thienopuridine compound. prodrug
  • acts on receptor to irreversible block ability of ADP to activate receptors for TXA2/platelet activation (GPC:P2Y12).
  • orally active. long lasting platelet inhibition (7-10days)
  • slowly activated by multiple CYP enzymes (CYP2C19), 2 steps.
  • 85% to inactive metabolism.
  • use: prevent thrombosis after stroke, MI, TIA, vascular events, before/after PCI or CABG, during a. fib or unstable angina.
  • toxicity: hemorrhage, skin rashes, GI problems
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57
Q

Clozapine

A
  • low potency atypical antipsychotic
  • blocks 40-60% D2, and 70-90% 5-HT2A.
    • blocks D2, D3, D4, 5-HT2, 5-HT3, 5-HT4.
  • acute = tranquilizer
  • chronic = antipsychotic takes a few wks.
  • good for positive symptoms, a little for negative.
  • use: refractory schizophrenia
  • side effects: 1% risk agranulocytosis, drooling, ↓ risk suicide, sedation, 2-5% risk of seizures from ↓ seizure threshold.
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59
Q

Cocaine

A
  • inhibits DA reuptake in CNS.
  • rapidly penetrates BBB ⇒ elation and euphoria.
  • major drug of abuse.
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60
Q

Codeine

A
  • opioid analgesic.
  • morphine with 3-methoxy = prodrug.
    • demethylated by CYP2D6 to morphine
  • mild to mod agonist of mu opioid receptors.
  • modest abuse potential.
  • use: mild to mod pain (short term use), MI, acute dyspnea from heart failure, analgesia, anesthesia
  • side effects: nausea, vomiting, histamine release.
  • use in combo with aspirin or acetaminophen.
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61
Q

Colchicine

A
  • inhibits granulocyte migration and phagocytosis.
  • acts in 12-24 hrs.
  • use: gout.
  • side effects: nausea, vomiting, abd pain, diarrhea
  • _intoxication _⇒ bloody diarrhea, shock, hematuria
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62
Q

Colestipol

A
  • bile acid sequestrant
  • binds BA in gut, excreted in feces
  • ⇒ liver converts more cholesterol to BA ⇒ ↓ cholesterol ⇒ ↑ LDLR and ↓ metabolism of LDLR.
  • interferes with absorption of fat-soluble vitamins (A, D, E, K), digitalis, cholorthiazide
  • stagger giving drugs
  • side effects: steatorrhea, constipation, bloating
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62
Q

Colesevelam

A
  • bile acid sequestrant
  • binds BA in gut, excreted in feces
  • liver converts more cholesterol to BA ⇒ ↓ cholesterol ⇒ ↑ LDLR and ↓ metabolism of LDLR
  • ⇒ mild ↓ both fasting and post-prandial glucose
  • interferes with absorption of fat-soluble vitamins (A, D, E, K), digitalis, chlorothiazide
  • stagger giving these
  • side effects: steatorrhea, constipation, bloating
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62
Q

Coxibs

A
  • NSAID. inhibits COX2.
  • Celecoxib (Celebrex) and Rofecoxib
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62
Q

Cyclophosphamide

A
  • non-biologic DMARD
  • use: SLE
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63
Q

Dantrolene

A
  • direct acting
  • inhibits calcium release from sarcoplasmic reticulum
  • use: spastic condictions
  • side effects: hepatotoxicity
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64
Q

Darifenacin

A
  • selective inhibitor for M3
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66
Q

Desipramine

A
  • secondary amine TCA.
  • NE transporter inhibitor.
  • metabolite of imipramine.
  • alpha-2 autoreceptor desensitization with chronic use.
  • use: ADHD, cocaine withdrawal, chronic neuropathic pain syndromes, fibromyalgia, stress incontinence.
  • side effects: ↑ body temp, cognitive impairment, constipation, urinary retention, closed-angle glaucoma, ↓ seizure threshold, cardiotoxicity, weight gain, sedation, orthostatic hypotension.
  • overdose: agitation, delirium, seizure, coma, fatal cardiac arrhythmias
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67
Q

Detemir

A
  • long acting insulin. s.c.
  • onset 1-5 hr, no peak, lasts 12-24 hr.
  • use: type 1 DM
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68
Q

Dexamethasone

A
  • PLA2 inhibitor by chelation of substrate, lipocortins or annexins, COX2 expression.
  • long acting corticosteroid.
  • t1/2 = 24-72 hrs.
  • dexamethasone test: give high dose over 2 days.
    • suppression = Cushing disease.
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70
Q

Dextromethorphan

A
  • use: cough suppression.
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71
Q

Diclofenac

A
  • COX1 and COX2 inhibitor.
  • analgesic
  • ⇒ ↓ arachidonic acid release in leukocytes.
  • high concentration in synovial fluid.
  • use: RA.
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71
Q

Diazepam

A
  • centrally acting benzodiazepine, halogen group
  • rapid acting, lipid soluble.
  • metabolite = **desmethyldiazepam **⇒ oxazepam ⇒ liver ⇒ urinary excretion
  • enhances GABA-A ⇒ ↑ inward Ca conduction post-synaptically
  • use: **minor spasticity, **relief of anxiety, insomnia, sedation and amnesia before procedures, status epilepticus (drug of choice), muscle relaxation in neuromuscular disorders, ethanol/sedative-hypnotic withdrawal.
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73
Q

Digoxin

A
  • glycoside
  • direct ionotropic drug ⇒ ↑ cardiac contractility ⇒ ↑ ER ⇒ ↓ LV EDP, ↓ wall tension ⇒ ↓ O2 consumption
  • clears pulm venous circulation, ↓ dyspnea, ↓ O2 consumption
  • orally active, mimics Ca ⇒ ↑ dilation
  • inhibits Na K ATPase ⇒ ↑ intracellular Na ⇒ ↑ intracellular Ca ⇒** ↑ contractility, ↑ active tension.**
  • renal elimination
  • oral bioavailabiliity = 55-65%, t1/2 = 36 hr.
  • CNS stimulant ⇒ ↑ parasympathetic and ↑ sympathetic (toxic levels) outlfow ⇒ ↓ HR, ↑ filling time, slower repolarization rate, prolonged refractory time, ↑ automaticity in atria/ventricles, ↓ conduction veocity in SA node, atria, AV node, ventricles, can ⇒ PVC.
  • use: CHF (stages C and D), bridge to transplant.
  • no tolerance, monitoring required
  • drug interactions: amiodarone, verapamil, quinidine, macrolide antibiotics, tetracyclines
  • toxicity: bradycardia, PVC, bigeminy, a. fib, a. flutter, paroxysmal SVT, AV blockade, abnormal color perception, fatigue, anxiety, nightmares.
  • tx for toxicity: discontinue, monitor K, check Ca intake, give lidocaine or phenytoin or digitalis Ab
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73
Q

Diltiazem

A
  • bezothiazipine CCB
  • binds at different site than verapamil
  • affects inner aspect of Ca channel, affects gating mechanism
  • ⇒ ↓ SA node rate, ↑ refractory period, ↑ PR interval
  • use: effort induced angina
  • side effects: peripheral edema, hypotension, tachycardia, palpitations, flushing, headaches, dizziness, nausea
  • use with beta blocker ⇒ severe bradycardia, AV block (reverse with atropine, Ca gluconate, glucagon, isoproterenol)
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74
Q

Diphenhydramine

A
  • antimuscarinic.
  • improves tremor and rigidity, little effect on bradykinesia.
  • use: add on for Parkinson’s Disease
  • side effects: sedation, dry mouth, etc. (anti-muscarinic effects)
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75
Q

Dipyridamole

A
  • ⇒ dilation of restrictive vessels
  • pressure on normal side to equal pressure on ischemic side = equalized pressure
  • myocardial steal/coronary steal causes blood to go to non-ischemic side (normal side)
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76
Q

Disopyramide

A
  • class IA Na channel blocker, anti-arrhythmetic
  • ↓ conduction velocity
  • convert unidirectional to bidirectional blockade, prolongs refractory period (K channel blocker), raises membrane threshold for excitation
  • use: supraventricular and ventricular arrhythmia
  • toxicity: ↑ ventricular rate, ↓ cardiac contractility, AV block, torsade de pointe, SA arrest, v tach, v fib
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77
Q

Dobutamine

A
  • alpha-1 beta-1 beta-2 agonist
  • best for beta-1
  • ⇒ ↑ HR and contractility
  • use: acute treatment of cardiac decompensation after heart surgery, or CHF
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77
Q

Donepezil

A
  • AchE inhibitor
  • ⇒ modest improvement in mild to mod Alzheimer’s.
  • positive effects at low doses
  • use: Alzheimer’s Disease
  • side effects: cholinergic side effects
    disease continues to progress
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78
Q

Doxazosin

A
  • alpha1 antagonist
  • alpha1>>>>alpha2
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78
Q

Dopamine

A
  • catecholamine ⇒ ↑ cardiac contractility by beta-1, water and Na diuresis by vasodilating vascular bed
  • relaxes splanchnic circulation
  • use: critical care, post-cardiac surgery, post-MI
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79
Q

Duloxetine

A
  • SNRI.
  • blocks NE and 5-HT reuptake.
  • activating agent.
  • use: depression and chronic pain disorders.
  • side effects: GI discomfort, sexual dysfunction, insomnia, tremor, acute anxiety.
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81
Q

Echothiophate

A
  • irreversible indirect acting organophosphate AChEI
  • itraocular route
  • use: glaucoma
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82
Q

Edrophonium

A
  • indirect acting, reversible AChEI
  • works at anionic site
  • short half life, use via IV
  • used in tensilen test to diagnose myasthenia gravis and ileus
  • enhances depolarization block
  • use: supraventricular tachycardia
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83
Q

Enalapril

A
  • alkyl ACEI.
  • short acting
  • give 1-2 times per day
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84
Q

Ephedrine

A
  • can cross BBB
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85
Q

Epinephrine

A
  • alpha-1, alpha-2, beta-1, beta-2 agonist
  • ⇒ ↑ HR, ↑ BPsys, ↓ BPdia, ↓ TPR
  • low/med dose ⇒ mostly beta-2 effect
    • alpha-1 ⇒ vasoconstriction, ↑ TPR
    • beta-1 ⇒ ↑ HR ⇒ ↑ CO ⇒ ↑ BPsys
    • beta-2 ⇒ vasodilation, ↓ BPdia
  • high dose ⇒ mostly alpha-1 effect
    • acts like NE
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85
Q

Eptifabatide

A
  • synthetic peptide fragment blocks GpIIb/IIIa receptor.
  • inhibits fibrinogen-dependent aggregation of activated platelets.
  • use: clot prevention during PCI and prevent restenosis after PCI.
  • toxicity: bleeding
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86
Q

Escitalopram

A
  • best tolerated SSRI
  • isomer of citalopram
  • selective 5-HT reuptake inhibitor.
  • minimal sedation, minimal weight gain, minimal autonomic effects.
  • 2nd longest half life.
  • use: depression (1st line), GAD, OCD, phobias, bulimia, pre-menstrual dysphoric disorder, perimenopausal symptoms
  • side effects: GI discomfort, sexual dysfunction, insomnia, tremor, acute anxiety.
  • discontinuation syndrome if stop suddenly = jittery, anxious, restless.
  • little chance of overdose.
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87
Q

Esmolol

A
  • aka Breviboc
  • beta-1 antagonist.
  • short duration = 10 min
  • popular in surgical procedures
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88
Q

Esomeprazole

A
  • proton pump inhibitor.
  • inhibits CYP2C19
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89
Q

Eszopiclone

A
  • aka Lunesta
  • selective benzodiazepine receptor agonist
  • t1/2 = 6 hours
  • minor active metabolites.
  • binds BDZ1 receptor
  • shortens sleep latency and ↑ total sleep
  • tolerance is rare.
  • use: hynotics (sedation), prevent jet lag.
  • side effects: rebound insomnia when stopping.
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90
Q

Etanercept

A
  • aka Enbrel
  • fusion protein: Fc portion of human IgG1 and TNFR2 receptor chains.
  • binds TNF, makes it inactive
  • binds LT (TNFbeta) that binds the same receptor.
  • shorter t1/2 than natural IgG1 Ab.
  • t1/2 of TNF complexes longer than free TNF.
  • use: RA, psoriasis, chronic juvenile arthritis, ankylosing spondylitis, psoriatic arthritis, uveitis.
    • use with methotrexate in RA
  • side effects: bacterial infections, TB, opportunistic infections (histo or coccidiomycosis), may ↑ mortality in CHF.
  • careful when giving to those with demyelinating diseases and SLE.
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91
Q

Ethacrynic Acid

A
  • loop diuretic
  • aka Edecrin
  • prodrug, adducts with cysteine group on methylene group
  • no sulfonamide group, has vinyl group
  • bound to plasma proteins, filtration enhanced by proteinuria
  • secreted by S2 segment of proximal tubules
  • acts from luminal side of TAL
  • given orally or IV
  • orally: onset of action = 30 min -1hr, duration = 6-8 hr
  • IV: onest of action = immediate, duration = 2hr
  • inhibits NKCC2 ⇒ ↓ lumen pos. potential ( back-leak of K into lumen) ⇒ ↑ Na, K, Cl in urine, ↓ resoprtion Ca, Mg.
  • ⇒ ↓ venous capacitance, ↓ concentrating ability (↓ NaCl reabsorption in medullary TAL), ↓ diluting ability (↓ NaCl resoprtion in cortical TAL), ↑ RBF and GFR
  • ⇒ ↑ Na and Cl excretion (Cl>Na), ↑ urine volume, isosthenuria, ↑ Ca and Mg excretion, ↑ PG and renin release, ↑ venous capacitance, block tubuloglomerular feedback, kaliuresis, ↓ osmotic gradient in medulla
  • uses: acute PE - ↓ pulm wedge pressure, ↓ LV filling pressure, in anephric pts, long term benefit, ↑ venous capacitance rapidly
    • edematous conditions: CHF, liver cirrhosis, nephritic syndrome, chronic heart failure, acute renal failure
    • acute hypercalcemia
    • hyperkalemia
    • acute renal failure
    • anion overdose
    • HTN
  • side effects: hypokalemic metabolic alkalosis, ototoxicity, hyperuricemia, hypomagnesia, allergic rxn, dehydration, hyperglycemia
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92
Q

Ethosuximide

A
  • closes T type Ca channels
  • serum levels may be ↑ by valproic acid.
  • use: absence seizures (drug of choice)
  • side effects: dizziness, GI distress, drowsiness, nausea.
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94
Q

Exenatide

A
  • GLP-1 resistant to DDP-4
  • causes weight loss.
  • use: type II DM with metformin or SU.
  • toxicity: ↑ risk hypoglycemia with SU, GI discomfort, pancreatitis.
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95
Q

Exetimibe

A
  • cholesterol absorption inhibitor ⇒ ↓ LDL.
  • inhibits intestinal cholesterol absorption from diet and bile, enter enterohepatic circulation
  • long t1/2 = 22 hr
  • ⇒ ↓ LDL (18%), synergistic with statins ⇒ ↑ LDLR and ↓ metabolism of LDLRs.
  • does not block bile acid absorption from gut
  • toxicity: low incidence of liver impairment
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96
Q

Febuxostat

A
  • non-competitive inhibitor Xanthine oxidase.
  • irreversibly inhibits.
  • ⇒ ↑ excretion uric acid.
  • use: gout
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97
Q

Fenofibrate

A
  • fibric acid derivative
  • ⇒ ↓ triglyceride levels in blood, ↑ activity LPL (TG lipase) ⇒ ↑ HDL, ↓ VLDL and IDL, ↓ LDL
  • known for PPAR alpha agonism
  • use: types IV and V hyperlipoproteinemia
  • toxicity: myopathy, rashes, ↑ incidence of gallstones, ↑ effect of warfarin (displaces from plasma protein binding)
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98
Q

Fentanyl

A
  • most potent opioid analgesic (100x morphine)
  • strong agonist of mu opioid receptors.
  • highly lipophilic, very fast across BBB.
  • IV lasts 15-30 min, SC or IM lasts 1-1.5 hrs, transdermal lasts 72 hrs.
  • ↑ risk overdose.
  • dose limiting respiratory depression.
  • high potential for abuse/dependence.
  • use: mod to severe pain. conscious sedation with medazolam, **pain in opioid tolerant pts **(transdermal), MI, acute dyspnea from heart failure, analgesia, anesthesia
  • side effects: respiratory depression
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99
Q

Flecainide

A
  • class IC Na channel blocker anti-arrhythmic drug
  • ⇒ ↓ conduction velocity.
  • marked widening of QRS interval
  • use: supraventricular and ventricular arrhythmias
  • may induce arrhythmias thru unidirectional block in normal cells.
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101
Q

Fludrocortisone

A
  • short-acting mineralcorticoid.
  • t1/2 = 8-12 hr.
  • use: acute adrenocortical insufficiency, Addison’s disease.
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101
Q

Fluoxetine

A
  • SSRI, longest t1/2 = 72 hrs.
  • selective 5-HT reuptake inhibitor.
  • can inhibit metabolism of other drugs via CYP450.
  • minimal sedation, weight gain, autonomic effects.
  • use: depression (1st line), GAD, OCD, phobias, bulimia, perimenopausal symptoms, pre-menstrual dysphoric disorder.
  • side effects: GI discomfort, sexual dysfunction, insomnia, tremor, acute anxiety.
  • discontinuation syndrome if stop suddenly = jittery, anxious, restless.
  • little chance of overdose.
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102
Q

Fluphenazine

A
  • high potency typical antipsychotic.
  • blocks D2
  • use low doses, milder sedation
  • use: schizophrenia
  • side effects: tardive dyskinesia, akathisia, parkonsonism, acute dystonia, hyperprolactinemia.
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103
Q

Fluticasone

A
  • inhaled corticosteroid
104
Q

Fluvastatin

105
Q

Formoterol

A
  • long acting beta agonist.
  • ↑ risk asthma related death.
  • use with corticosteroids.
106
Q

Furosemide

A
  • loop diuretic
  • aka Lasix
  • has sulfonamide group
  • bound to plasma proteins, filtration enhanced by proteinuria
  • secreted by S2 segment of proximal tubules
  • acts from luminal side of TAL
  • dosage: 20-40mg
  • given orally or IV
    • orally: onset of action = 30 min -1hr, duration = 6-8 hr
    • IV: onest of action = immediate, duration = 2hr
  • inhibits NKCC2 ⇒ ↓ lumen pos. potential ( back-leak of K into lumen) ⇒ ↑ Na, K, Cl in urine, ↓ resoprtion Ca, Mg.
  • ⇒ ↓ venous capacitance, ↓ concentrating ability (↓ NaCl reabsorption in medullary TAL), ↓ diluting ability (↓ NaCl resoprtion in cortical TAL), ↑ RBF and GFR
  • ⇒ ↑ Na and Cl excretion (Cl>Na), ↑ urine volume, isosthenuria, ↑ Ca and Mg excretion, ↑ PG and renin release, ↑ venous capacitance, block tubuloglomerular feedback, kaliuresis, ↓ osmotic gradient in medulla
  • uses: acute PE - ↓ pulm wedge pressure, ↓ LV filling pressure, in anephric pts, long term benefit, ↑ venous capacitance rapidly
    • edematous conditions: CHF, liver cirrhosis, nephritic syndrome, chronic heart failure, acute renal failure
    • acute hypercalcemia
    • hyperkalemia
    • acute renal failure
    • anion overdose
    • HTN
  • side effects: hypokalemic metabolic alkalosis, ototoxicity, hyperuricemia, hypomagnesia, allergic rxn, dehydration, hyperglycemia
107
Q

Gabapentin

A
  • aka Neurontin
  • GABA mimetic, attempt to make GABA lipophilic.
  • does NOT bind GABA A receptor.
  • releases GABA from GABA-ergic neurons, indirect acting.
  • additive with other CNS depressants.
  • renal clearance, ↓ dose with renal impairment.
  • use: all partial seizures, chronic pain, migraine prophylaxis.
  • side effects: ataxia, dizziness, tremor, drowsiness, nystagmus.
108
Q

Galantamine

A
  • AchE inhibitor
  • positive allosteric modulator of nicotinic Ach receptors
  • ⇒ modest improvement in mild to mod Alzheimer’s.
  • positive effects at low doses
  • use: Alzheimer’s Disease
  • side effects: cholinergic side effects
  • disease continues to progress
109
Q

Glargine

A
  • long acting insulin. s.c.
  • onset 1-2 hr, no peak, lasts >24hrs.
  • use: type 1 DM
110
Q

Glimepiride

A
  • SU, 2nd gen.
  • ⇒ mod ↓ both fasting and post-prandial glucose.
  • lasts 10-24 hr. liver metabolism.
  • binds SUR of KATP channel ⇒ depolarization, Ca influx, insulin release.
  • binds plasma protein
  • use: type II DM
  • don’t use: type I DM, pregnancy, stress, surgery, infection, renal/liver impairment.
  • side effects: hypoglycemia, weight gain, nausea, vomiting, GI discomfort
112
Q

Glipizide

A
  • SU. 2nd gen.
  • ⇒ mod ↓ both fasting and post-prandial glucose.
  • lasts 10-24 hr. liver metabolism.
  • binds SUR of KATP channel ⇒ depolarization, Ca influx, insulin release.
  • binds plasma protein
  • use: type II DM
  • don’t use: type I DM, pregnancy, stress, surgery, infection, renal/liver impairment
  • side effects: hypoglycemia, weight gain, nausea, vomiting, GI discomfort.
113
Q

Glucocorticoids

A
  • CYP3A4 inducer
  • use: osteoarthritis, RA, SLE.
114
Q

Glulisine

A
  • rapid acting insulin
115
Q

Glycopyrrolate

A
  • quaternary amine.
  • use: GI hypermotility
115
Q

Glyburide

A
  • SU. 2nd gen.
  • ⇒ mod ↓ both fasting and post-prandial glucose.
  • lasts 10-24 hr
  • mild diuretic, metabolized by liver.
  • bind SUR of KATP channel ⇒ depolarize, Ca influx, insulin release.
  • binds plasma protein
  • use: type II DM
  • don’t use: type I DM, pregnancy, stress, surgery, infection, renal/liver impairment.
  • side effects: hypoglycemia, weight gain, nausea, vomiting, GI discomfort.
116
Q

Haloperidol

A
  • high potency typical antipsychotic.
  • inhibits D2 and other receptors.
  • acute = tranquilizing effects but still psychosis.
  • chronic = antipsychotic effects after 2-4 wks.
  • use: schizophrenia, particularly in emergencies and in pregnancy, Tourette’s syndrome, Huntington’s chorea.
  • side effects: tardive dyskinesia, parkinsonism, akathisia, acute dystonia, hyperprolactinemia.
118
Q

Halothane

A
  • halogenated inhaled anesthetic
119
Q

Homatropine

A
  • muscarinic antagonist.
  • atropine with -OH
120
Q

Hydralazine

A
  • can ⇒ symptoms that look like Lupus.
  • involves heart, arthritis, maybe renal.
  • only Ab to ssDNA.
  • in ppl that are slow acetyators.
  • dilates arterioles ⇒ ↑↑↑ CO
121
Q

Hydrochlorothiazide

A
  • thiazide diuretic
  • 10x more potent than chlorothiazide
  • inhibits NCC in distal convoluted tubule ⇒ ↓ intracellular Na ⇒ slowed Na K ATPase ⇒ absorb Ca ⇒ hypocalcuria
  • ↓ ability to produce dilute urine, ↓ free water formation
  • uses: edema from CHF, HTN, calcium nephrolithiasis and osteoporosis,
    • mainstay for: nephrogenic diabetes insipidus*****
  • side effects: extracellular volume depletion, hypotension, hypokalemia, dilutional hyponatremia, ↓ glucose tolerance, hyperlipidemia, allergic rxns (sulfonamide group), ↑ risk digoxin toxicity, ↑ risk quinidine-induced torsades de pointes.
122
Q

Ibuprofen

A
  • NSAID. inhibits COX1 and COX2.
  • analgesic, antipyretic, anti-inflammatory.
  • better tolerated than aspirin.
  • longer t1/2
  • contraindicated in nasal polyps.
  • side effects: GI ulceration, hemorrhage, renal toxicity.
122
Q

Ibandronate

A
  • bisphosphonate, oral.
  • inhibits FPPS ⇒ ↓ cholesterol, ↓ osteoclast survival.
  • poorly absorbed.
  • take before meals.
  • ⇒ ↓ risk spine and hip fractures.
  • use: osteoporosis
  • side effects: GI irritation, osteonecrosis
123
Q

Imipramine

A
  • tertiatry amine TCA.
  • antagonist at alpha1, muscarinic and histaminergic H1 receptors.
  • inhibits NE and 5-HT reuptake pumps.
  • blocks fast-Na channels.
  • active metabolite = desipramine
  • use: bed-wetting.
  • side efects: dry mouth, constipation, blurred vision, orthostatic hypotension, difficulty urinating, sedation, confusion, weight gain, prolonged QT with cardiac toxicity in overdose.
  • overdose: agitation, delirium, seizure, coma, fatal cardiac arrhythmias
124
Q

Indomethacin

A
  • NSAID. inhibits COX1.
  • analgesic, antipyretic (Hodgkin’s disease), anti-inflammatory.
  • inhibits urate crystal phagocytosis.
  • use: PDA, acute gouty arthritis, acute inflammation.
  • side effects: GI ulcers, renal toxicity.
125
Q

Infliximab

A
  • aka Remicade
  • give IV
  • chimeric monoclonal Ab against TNF (mouse and human)
  • does not bind LT
  • binds transmembrane TNF, TNF monomer, and active trimer
  • ⇒ caspase-3 activation and apoptosis of activated lymphocytes, reverse signaling via mTNF.
  • ⇒ ↓ number of swollen joints and severity of RA. blocks granulocyte migration into joint, ↓ circulating VEGF.
  • use: with methotrexate in refractory RA, Crohn’s disease. also juvenile chronic arthritis, ankylosing spondylitis, psoriasis, psoriatic arthritis, uveitis, IBD.
  • side effects: bacterial infections, TB, opportunistic infections (histo or coccidiomycosis), ↑ mortality with CHF.
  • be careful when using with demyelinating disease and SLE.
126
Q

Insulin

A
  • short acting.
  • onset 30 min, peak 2-3 hr, lasts 5-10 hr.
  • ⇒ ↓ fasting and post-prandial glucose
  • use: type 1 DM
  • side effects: hypoglycemia, weight gain, lipohypertrophy, lipodystrophy, insulin edema, allergic rxn, insulin resistance.
127
Q

Ipratropium

A
  • non-selective anticholinergic
  • quaternary salt, doesn’t cross BBB
  • slow onset: 1-2 hrs.
  • duration: 6-8hrs.
  • ⇒ reverse bronchoconstriction.
  • additive effect with beta agonists.
  • use: COPD
128
Q

Isocarboxazid

A
  • MAOI
    • irreversibly inhibits MAO-A and MAO-B.
  • use: depression when can’t take other drugs from toxicity.
  • side effects: weight gain, postural hypertension, sexual dysfunction, altered sleep.
  • hypertensive crisis: if take with foods containing tyramine or OTC decongestants (phenylephrine or pseudoephedrine)
  • serotonin syndrome = rigidity, hyperthermia, altered mental status, cardiovascular collapse.
    • if taking SSRIs, meperidine, or dextromethorphan.
  • overdose: CNS intoxication (agitation, delirium, seizures, coma). can be fatal.
129
Q

Isoproterenol

A
  • beta-1 = beta-2 agonist
  • beta-1 ⇒ ↑ HR ⇒ ↑ CO ⇒ ↑ BPsys
  • beta-2 ⇒ ↓ TPR ⇒ ↓ BPdia
  • for beta-2, iso>epi>>NE
130
Q

Isosorbide

A
  • osmotic diuretic
  • orally active
132
Q

Isosorbide Dinitrate

A
  • organic nitrate ⇒ 2NO
  • metabolized by liver, low bioavailability
  • low dose ⇒ dilate venous side.
  • high dose ⇒ ↓ arteriolar resistance and ↓ coronary afterload
  • ⇒ ↓ myocardial O2 demand
  • relaxes large coronary vessels and collateral vessels ⇒ ↑ collateral blood flow ⇒ ↓ systolic and diastolic BP ⇒ ↑ blood to subendocardium, ↓ platelet aggregation, some ↑ symp output ⇒ ↑ cardiac contractility so CO doesn’t ↓
  • causes: ↓ wall tension, ↓ LV EDV and pressure ⇒ ↓ myocardial O2 use, vasodilation, ↑ epicardiac artery size, ↑ coronary blood flow, ↓ aortic pressure
  • use: effort induced angina
  • side effects: orthostatic hypotension, tachycardia, headache, tolerance
133
Q

Ketorolac

A
  • analgesic
  • replaces morphine after surgery
133
Q

Ketoprofen

A
  • NSAID. reversibly inhibits COX1 and COX2.
  • analgesic, antipyretic, anti-inflammatory.
  • better tolerated than aspirin.
  • longer t1/2.
  • not used for nasal polyps.
  • side effects: GI ulcers, hemorrhage, renal toxicity.
134
Q

L-DOPA

A
  • converted by DOPA-decarboxylase to DA.
  • ⇒ ↑ DA release by surviving neurons.
  • need higher dose as disease progresses
  • use: Parkinson’s Disease.
  • side effects: nausea, vomiting, ↑ risk dyskinesias, GI adverse effects, postural hypotension, depression, hallucination, anxiety, agitation.
  • 80% get dyskinesias with long term use.
  • may hasten disease progression.
136
Q

Labetolol

A
  • alpha-1, alpha-2, beta-1, beta-2 antagonist
  • beta-1 = beta-2 >or= alpha-1 > alpha-2
  • must discontinue slowly
  • danger for organ damage
  • use: short to HTN crisis
137
Q

Lamotrigine

A
  • prolongs inactivation of Na channel.
  • use: simple partial seizures, complex partial seizures, tonic-clonic seizures, acute manic episodes and prophylaxis.
138
Q

Latanoprost

A
  • PFG2 analog.
  • use: glaucoma, ocular HTN
139
Q

Lidocaine

A
  • Class IB Na channel blocker, anti-arrhythmic drug
  • amide local anesthetic
  • ⇒ ↑ conduction velocity.
  • metabolized by microsomal hydrolases
  • blocks Na channels from inner aspect of membrane.
  • needs to be lipophilic to get into axoplasm
  • needs to be cationic to get to Na channel.
  • use: ventricular arrhythmias, supraventricular and ventricular arrhythmias from digitalis.
  • toxicity: CNS sedation at therapeutic levels (restlessness, tremor, convulsions), **excitation then depression at higher levels, ↓ AV conduction, ↓ automaticity (prevent ventricular escape), cardio = vasodilation, hypotension, ↓ excitability of cardiac muscle, ↓ conduction velocity, ↓ force of contraction **
139
Q

Levothyroxine

A
  • T4.
  • 80% bioavailability
  • t1/2 = 7 days
  • start immediately
  • use: hypothyroidism
  • in elderly, if have angina or cardiac arrhythmia then ↓ dose.
141
Q

Liraglutide

A
  • GLP-1 analog
  • sc 1x a day
  • add on to metformin or SU.
  • use: type II DM
  • toxicity: pancreatitis, ↑ risk hypoglycemia with SU, GI discomfort
141
Q

Lisinopril

A
  • ACEI
  • long acting
  • 1-2 times per day
143
Q

Lispro

A
  • rapid acting insulin. s.c.
  • onset 5-15 min, peak 1 hr, lasts 3-5 hr.
  • use: type 1 DM
  • side effects: hypoglycemia, weight gain, lipohypertrophy, lipodystrophy, insulin edema, allergic rxn, insulin resistance.
143
Q

Lithium Carbonate

A
  • monovalent cation similar to Na.
  • impairs inositol recycling by inhibiting phosphatases
  • give orally, absorbed in 6-8 hrs.
  • plasma serum peaks in 30min to 2 hrs, t1/2 = 20 hrs..
  • excreted in urine, can be reabsorbed.
  • decrease dose if on thiazide or loop diuretic.
  • narrow therapeutic index (0.6-1.4).
  • use: bipolar disorder.
  • side effects: excessive thirst, polyuria, memory problems, tremor, weight gain, drowsiness, diarrhea.
  • toxicity: nausea, vomiting, diarrhea, ataxia, confusion, coma, convulsions, death. irreversible brain damage.
  • usually combine with atypical antipsychotic.
144
Q

LMW Heparin

A
  • ex: enoxaparin, dalteparin, danaproid
  • ATIII-dependent. selectively inhibits factor Xa.
  • give IV or s.c.
  • longer t1/2 than heparin (2x)
  • renal clearance
  • safe during pregnancy
  • use: acute/chronic tx of arterial/venous thrombosis, clot prevention
  • toxicity: hemorrhage, osteoporosis (chronic), heparin-induced thrombocytopenia (HIT)
145
Q

Loperamide

A
  • synthetic opioid. related to meperidine.
  • mild to mod agonist of mu opioid receptors.
  • low aqueous solubility.
  • poorly absorbed orally, doesn’t cross BBB well.
  • works best in GI tract with no CNS effects.
  • no abuse potential.
  • use: diarrhea
146
Q

Lorazepam

A
  • benzodiazepine, halogen group
  • ⇒ liver ⇒ urinary excretion
  • no active metabolites.
  • longer period of protection for status epilepticus than diazepam
  • use: relief of anxiety, insomnia, sedation and amnesia before procedures, epilepsy and seizure states (status epilepticus), muscle relaxation in neuromuscular disorders, ethanol/sedative-hypnotic withdrawal.
147
Q

Lovastatin

A
  • from mold. exists as lactone or free acid
  • free acid competes with HMG-CoA reductase and blocks synthesis of cholesterol at rate limiting step
  • works thru CYP3A4
    • inhibited b grapefruit, erythromycin, ketoconazole
149
Q

Melocicam

A
  • COX2 inhibitor.
149
Q

Mannitol

A
  • osmotic diuretic
  • does not cross water permeable membranes, ↓ fluid reabsoprtion (proximal tubules, thick ascending limb)
  • IV only
  • causes water to leave cells, keeps nephrons patent.
  • freely filtered, not reabsorbed by kidney.
  • uses: ↓ intraocular pressure in glaucoma, ↓ intracerebral pressure, anuria states (rhabdomyolysis)
  • side effects: hypovolemia
  • contraindications: CHF = ↓ kidney function so not filtered ⇒ hyponatremia, hypervolemia
150
Q

Memantine

A
  • NMDA receptor, negative allosteric modulator
  • use: mod to severe Alzheimer’s Disease
  • small benefit
  • disease still progresses
151
Q

Meperidine

A
  • synthetic opioid analgesic.
  • strong agonist of mu opioid receptors.
  • extensive 1st pass metabolism
  • more lipophilic so crosses BBB, duration = 2-4 hrs.
  • ester hydrolysis ⇒ meperidinic acid (inactive and eliminated).
  • slower demethylation ⇒ normeperidine = toxic ⇒ delirium, seizures.
    • higher in pts with renal insufficiency or dehydration.
  • dose limiting respiratory depression.
  • high potential for abuse/dependence.
  • use: mod to severe pain, childbirth, MI, acute dyspnea from heart failure, analgesia, anesthesia, post anesthesia shivering
  • side effects: respiratory depression
152
Q

Mepivacaine

A
  • amide local anesthetic.
  • metabolized by microsomal hydrolase
  • blocks Na channel from within axoplasm.
  • toxicity: CNS = depress inhibitory neurons ⇒ restlessness, tremor, convulsions.
    • cardio = vasodilation, hypotension, ↓ excitability of cardiac muscle, ↓ conduction velocity, ↓ force of contraction.
  • death by respiratory failure
153
Q

Metformin

A
  • activates AMPK
  • ⇒ mod ↓ fasting glucose, mild ↓ post-prandial glucose, ↓ hepatic glucose output (↓ gluconeogenesis, ↓ glycogenolysis)
  • ↑ peripheral glucose uptake, ↓ insulin resistance.
  • weight neutral, ↓ CV risk, ↓ triglycerides, ↓ cholesterol
  • euglycemic.
  • renal elimination
  • use: infertility, type II DM.
  • don’t use: renal/liver impairment, alcohol abuse, heart and resp insuffieciency or hypoxia.
  • side effects: anorexia, nausea, vomiting, lactic acidosis
154
Q

Methacholine

A
  • good muscarinic activity
  • no nicotinic activity
  • slightly susceptible to AChE
  • use: glaucoma
156
Q

Methimazole

A
  • inhibits TPO, antithyroid drug
  • use after 1st trimester in pregnancy
  • less hepatotoxicity
  • use: hyperthyroidism
  • side effects: rash, nausea, GI discomfort, agranulocytosis
156
Q

Methadone

A
  • synthetic opioid analgesic.
  • strong agonist of mu opioid receptors.
  • good oral bioavailability (slow hepatic metabolism)
  • easily penetrates BBB, duration = 4-6 hrs.
  • accumulates in tissues with chronic dosing from high protein binding.
  • can prevent drug craving or withdrawal.
  • dose limiting respiratory depression.
  • high potential for abuse/dependence.
  • use: mod to severe pain, chronic maintenance of opioid addicts, MI, acute dyspnea from heart failure, analgesia, anesthesia
  • side effects: respiratory depression
157
Q

Methotrexate

A
  • non-biologic DMARD
  • folate analog = blocks tetrahydrofolate-dependent steps in purine metabolism
  • lower doses = anti-inflammatory
  • high doses = cytotoxic (chemo)
  • ↑ adenosine formation ⇒ anti-inflammatory via **A2a and A2b receptors **⇒ ↑ cAMP
  • ⇒ ↓ IL-1 and IL-6; ↑ monocyte apoptosis, ↑ IL-1ra, ↑ IL-4 and IL-10, inhibit COX2 synthesis and neutrophil chemotaxis
  • use: first line for RA
  • side effects: hair loss, nausea, headaches, skin pigmentation
159
Q

Metoclopramide

A
  • promotes stomach emptying
160
Q

Metoprolol

A
  • **beta-1 antagonist **
  • ↓ renin release, ↓ HR, ↓ myocardial O2 consumption, ↓ downregulation of beta receptors
161
Q

Mevostatin

A
  • 1st statin discovered.
  • from mold
162
Q

Midazolam

A
  • use: conscious sedation, pre-medication for monitored anesthesia
163
Q

Miglitol

A
  • inhibits alpha-glucosidase, inhibits breakdown of starches, saccharides
  • delays glucose absorption in SI.
  • insulin-sparing.
  • take before meals.
  • side effects: flatulence, diarrhea, abd pain, ↑ risk hypoglycemia in pt with SU
163
Q

Mirtazapine

A
  • atypical antidepressant.
  • blocks alpha-2 and 5-HT2A.
  • no sexual side effects.
  • well tolerated by elderly.
  • does not ↑ seizure risk, safe from overdose
  • use: depression
  • side effect: 0.3% chance agranulocytosis, sedation, weight gain.
165
Q

Misoprostol

A
  • PGE1 analog
  • use: early abortion, tx of miscarriage, prevent NSAID-induced peptic ulcer.
166
Q

Mivacurium

A
  • competitive NMJ blocking agent.
  • large and bulky
  • inhibits amplitude of endplate potentials so propagated action potential can’t develop
  • causes ++ histamine release
  • duration: 10-15 min
  • elimination: plasma pseudocholinesterase
  • use: muscle relaxant, anesthetic
  • side effects: autonomic
  • reversed by ACHEI and ↑ extracellular K+
167
Q

Montelukast

A
  • leukotriene receptor blocker
  • use: asthma, allergic rhinitis
168
Q

Morphine

A
  • opioid analgesic.
  • strong agonist of mu opioid receptors.
  • low bioavailability orally (25%). so give SC, IM, or IV.
    • rapid analgesia, duration = 4-5 hrs.
    • metabolized in liver to C3 or C6 glucuronic acid.
      • C6 is still analgesic and can accumulate with chronic use and slow clearance.
    • excreted in urine.
  • low lipophilicity so need high plasma concentration to cross BBB.
  • dose limiting respiratory depression.
  • high potential for abuse/dependence.
  • use: IM or IV for mod to severe pain, orally for chronic therapy, MI, acute dyspnea from heart failure, analgesia, anesthesia
  • side effects: respiratory depression
169
Q

Na Nitroprusside

A
  • cardiac unloading agent.
  • ⇒ ↑ sympathetic outlfow
  • ⇒ NO spontaneously.
  • dilates arterioles ⇒ ↓↓ LV EDP, ↑↑ CO, ↓ BP
170
Q

Nabumetone

A
  • NSAID. inhibits COX2.
171
Q

Naproxen

A
  • NSAID. reversibly inhibits COX1 and COX2.
  • analgesic, antipyretic, anti-inflammatory.
  • better tolerated than aspirin.
  • longer t1/2
  • not used for nasal polyps.
  • side effects: GI ulcers, hemorrhage, renal toxicity.
172
Q

Neostigmine

A
  • indirect acting carbamate AChEI, competitive reversible
  • works at anionic and esteratic sites
  • oral, subQ routes, 1-3 hrs.
  • does not cross BBB
  • enhances depolarization block
  • use: neurogenic ileus, myasthenia gravis, urinary retention
173
Q

Nifedipine

A
  • DHP CCB. powerful arterial dilator
  • affects outer aspect of Ca channel, plugs selectivity filter.
  • could cause negative inotropic, chronotropic, dromotropic activity
  • ⇒ ↑ HR from sympathetic reflex.
  • use: with alpha blockers for profound ↓ arterial BP, shock.
  • side effects: peripheral edema, hypotension, tachycardia, palpitations, flushing, headaches, dizziness, nausea
  • 1st dose is 1/2 - 1/4 normal dose since may cause hyper-response and impair blood flow
173
Q

Niacin

A
  • Nicotinic acid, Vit B. water soluble vitamin
  • high doses = works as lipophilic drug
  • blocks release of VLDL in liver ⇒ ↓ triglyceride levels and IDL and LDL levels, ↑ HDL, ↓ Lp(a) (thrombogenic lipoprotein in metabolic syndrome)
  • inhibits CETP ⇒ ↑ HDL, prevents HDL from going into VLDL molecule.
  • use: ↑ TGs or ↑ cholesterol, types II and IV hyperlipoproteinemia.
  • give with statin for type IIb
  • side effect: facial flushing from PGD2 release, tachyphylaxis, hepatic toxicity, GI irritation, ↓ glucose tolerance
  • patch = ↓ flushing but ↑ hepatotoxicity
175
Q

Nimodipine

A
  • CCB.
  • given IV
  • lipophilic, crosses BBB
  • use: SAH from burst cerebral aneurysm
  • ⇒ ↓ neurological deficit
176
Q

Nitroglycerin

A
  • 3NO, vasodilation and anti-platelet activation
  • low dose ⇒ venous dilation
  • high dose ⇒ ↓ arteriolar resistance, ↓ coronary afterload ⇒↓ myocardial O2 demand
  • duration = 10-30 min
  • do not give orally
  • relaxes large coronary vessels and collateral vessels ⇒ ↑ collateral blood flow ⇒ ↓ syst and diast BP ⇒ ↑ blood flow to subendocardium, ↓ platelet aggregation. some ↑ symp output ⇒ ↑ cardiac contractility so CO doesn’t ↓.
  • exogenous NO ⇒ guanylyl cyclase ⇒ cGMP ⇒ ↓ wall tension, ↓ LV EDV and pressure ⇒ ↓ myocardial O2 consumption.
  • coronary vasodilation, ↑ epicardial artery size, ↑ coronary blood flow, ↓ aortic pressure. redistributes blood to ischemic side
  • use: effort-induced angina
  • side effects: orthostatic hypotension, tachycardia, headache, tolerance.
177
Q

Norepinephrine

A
  • alpha-1 alpha-2 beta-1 agonist
  • alpha-1>beta-1 effects ⇒ ↓ HR, ↑ BP
  • sympathetic withdrawal thru baroreceptors
  • NE ⇒ ↑ TPR, ↑ BP, ↓ HR
178
Q

NPH

NPL

NPA

A
  • immediate acting insulin
  • onset 2hr, peak 4-8hr, lasts 12-16 hr
  • use: type 1 DM
  • side effects: hypoglycemia, weight gain, lipohypertophy, lipodystrophy, insulin edema, allergic rxn, insulin resistance.
178
Q

Nortriptyline

A
  • secondary amine TCA.
  • metabolite of amitriptyline.
  • narrow therapeutic window.
  • less side effects than amitriptyline.
  • use: depression, chronic neuropathic pain syndromes, fibromyalgia, stress incontinence.
  • overdose: agitation, delirium, seizure, coma, fatal cardiac arrhythmias
180
Q

Ocreotide

A
  • long acting somatostatin agonist
  • inhibits GH>insulin
  • use: acromegaly, palliative for carcinoid syndrome (inhibits release 5HT, histamine, bioactive peptides), WDHA syndrome, hypoglycemia from sulfonylurea overdose
181
Q

Olanzapine

A
  • high potency atypical antipsychotic.
  • blocks 40-60% D2, and 70-90% 5-HT2A.
  • acute = tranquilizer
  • chronic = antipsychotic after a few wks.
  • good for positive symptoms, a little for negative.
  • use: schizophrenia, mood stabilizer, psychosis with manic-depressive/schizoaffective disorders or depression.
  • side effects: ↑ liver enzymes, drooling, sedation.
181
Q

Omalizumab

A
  • IgG1 monoclonal anti-IgE Ab
  • binds Fc region of IgE ⇒ ↓ free IgE, ↓ eosinophils in sputum and bronchial mucosa.
  • ⇒ early and late phase asthmatic rxn.
  • given s.c.
  • expensive
  • use: severe asthma
183
Q

Omeprazole

A
  • proton pump inhibitor
  • inhibits CYP2C19
183
Q

Ondansetron

A
  • 5-HT3 antagonist ⇒ antiemetic
184
Q

Opioid Overdose

A
  • coma
  • pinpoint pupils
  • depressed respiration
186
Q

Oxybutynin

A
  • M antagonist = M3
  • prevents urge incontinence for hyperactive bladder
186
Q

Oxazepam

A
  • benzodiazepine, halogen group
  • slow acting, slow absorption
  • ⇒ liver ⇒ urinary excretion
  • no metabolites.
  • use: relief of anxiety, insomnia, sedation and amnesia before procedures, epilepsy and seizure states, muscle relaxation in neuromuscular disorders, ethanol/sedative-hypnotic withdrawal.
187
Q

Oxytocin

A
  • acts on uterus and lactating mammary gland
  • use: induce labor, incomplete abortions, postpartum hemorrhage.
    • intranasal to aid lactation
  • toxicity: hemorrhage, trauma to neonate, ↑ BP
189
Q

Pancuronium

A
  • competitive NMJ blocking agent.
  • large and bulky
  • inhibits amplitude of endplate potentials so propagated action potential can’t develop
  • no histamine release
  • duration: hours
  • elimination: renal
  • use: muscle relaxant, anesthetic
  • side effects: blockade of nicotinic receptors in parasympathetic ganglia. (↑ HR, **↑ BP, **↑ AV conduction)
  • reversed by ACHEI and ↑ extracellular K+
191
Q

Paroxetine

A
  • SSRI, 2nd shortest t1/2.
  • selective 5-HT reuptake inhibitor.
  • can inhibit metabolism of other drugs by CYP450.
  • most sedating SSRI, causes weight gain.
  • slightly anticholinergic.
  • activating agent, can cause hyperactivity.
  • can cause extrapyramidal symptoms in schizophrenic pts.
  • use: depression (1st line), GAD, OCD, phobias, bulimia, pre-menstrual dysphoric disorder, perimenopausal symptoms.
  • side effects: GI discomfort, sexual dysfunction, insomnia, tremor, acute anxiety, anisocoria
  • discontinuation syndrome if stop suddenly = jittery, anxious, restless.
  • little chance of overdose.
192
Q

Pentobarbital

A
  • barbiturate
  • potentiate GABA at GABA-benzo-chloride channel.
  • short acting
  • metabolized in liver
  • induces CYTP450 metabolism of lipid-soluble drugs (oral BC, carbamazepine, phenytoin, warfarin)
  • chronic use ⇒ tolerance.
  • cross-tolerance btw benzo, barbiturates, ethanol.
  • use: NOT USED PORPHYRIAS
  • side effects: marked sedation, tolerance, respiratory depression
  • withdrawal: anxiety, agitation, life-threatening seizures
    • tx: supportive care, long acting benzo
193
Q

Phenelzine

A
  • MAOI
    • irreversibley inhibits MAO-A and MAO-B.
  • use: depression when can’t use other drugs from toxicity.
  • side effects: weight gain, postural hypertension, sexual dysfunction, altered sleep.
  • hypertensive crisis: if taking with foods containing tyramine or OTC decongestants (phenylephrine or pseudoephedrine).
  • serotonin syndrome = rigidity, hyperthermia, altered mental status, cardiovascular collapse.
    • if taking with SSRIs, meperidine, or dextromethorphan.
  • overdose: CNS intoxication (agitation, delirium, seizures, coma). can be fatal.
194
Q

Phenobarbital

A
  • CYP2C9 inducer
196
Q

Phenoxybenzamine

A
  • non-competitive irreversible alpha-1 alpha-2 antagonist.
  • alpha-1 > alpha-2
  • dilates arterioles and veins ⇒ ↓↓ LV EDP, ↑↑ CO, ↑ HR, ↓ BP
  • use: pheochromocytoma for HTN crisis
196
Q

Phentolamine

A
  • alpha-1 = alpha-2 antagonist
  • ↑ sympathetic outflow
  • dilates arterioles and veins ⇒** ↓↓ LV EDP, ↑↑ CO, ↓BP**
197
Q

Phenylephrine

A
  • alpha-1 agonist
  • ⇒ ↑ TPR ⇒ ↑ BP, ↓ HR
  • not recognized by COMT
199
Q

Physostigmine

A
  • irreversible indirect acting carbamide AChEI
  • works at anionic and esteratic sites
  • intraocular, IM, IV routes.
  • long lasting
  • crosses BBB
  • use: glaucoma, atropine intoxication
199
Q

Phenytoin

A
  • prolongs inactivated Na channel.
  • metabolized in liver: para-hydroxylation of phenyl groups.
    • induce metabolism: phenobarbital, carbamazepine
    • cause ↑ levels: chloramphenicol, dicumarol, cimetidine, sulfonamides, isoniazid
  • narrow therapeutic window.
  • painful when given IV.
  • use: status epilepticus, simple partial seizures, complex partial seizures, tonic-clonic seizures.
  • toxicity: diplopia, ataxia, gingival hyperplasia, hirsutism, coarsening of facial features.
200
Q

Pilocarpine

A
  • direct acting muscarinic agonist, alkaloid
  • oral and intraocular routes
  • resistant to AChE
  • ⇒ ↓ BP, no change HR, vasodilation
  • crosses BBB
  • use: glaucoma and Sjogren’s syndrome, hypotensive agent when IV.
201
Q

Pioglitazone

A
  • TZD. 2nd line, add on to metformin.
  • activates PPARgamma ⇒ ↑ insulin sensitivity
  • slow onset. euglycemic.
  • ⇒ ↓ fasting glucose, mild ↓ post-prandial
  • redistribute fat from visceral to subQ
  • ⇒ ↓ triglycerides, ↑ HDL, ↓ LDL
  • toxicity: weight gain, ↑ risk CHF, ↑ risk bone fractures, ↑ risk hypoglycemia with SU, ↑ risk bladder cancer.
203
Q

Pramlintide

A
  • ⇒ slow gastric emptying, inhibits glucagon release, ↑ satiety
  • short duration, give before meals
  • strong ↓ post-prandial glucose, mild ↓ fasting glucose.
  • causes weight loss.
  • use: type I and II DM who are insulin dependent, post-prandial hyperglycemia.
  • toxicity: ↑ risk hypoglycemia, GI discomfort.
203
Q

Pramipexole

A
  • non-ergot DA receptor agonist
    • preferred over ergots (faster and safer titration)
  • less motor recovery and more side effects than L-DOPA.
  • ↓ risk dyskinesias.
  • use: Parkinson’s Disease, restless-legs syndrome
  • side effects: nausea, vomiting, psychiatric rxns, postural hypotension, sudden onset daytime sleepiness
  • dose related effects eventually outweight therapeutic effects.
205
Q

Prasugrel

A
  • platelet inhibitor. prodrug
  • thienopuride compound.
  • inhibits ADP receptor of GPCR:P2Y12 irreversibly.
  • metabolized by CYP enzymes.
  • rapidly activated, give loading dose.
  • orally active. long lasting platelet inhibition (7-10days)
  • use: prevent thrombosis after MI, vascular events, before/after PCI or CABG, during a. fib or unstable angina.
  • not for stroke or TIA.
  • toxicity: hemorrhage, skin rashes, GI problems
206
Q

Prazosin

A
  • alpha-1 antagonist
  • ⇒ ↑ sympathetic flow
  • dilates arterioles ⇒ ↓↓ LV EDP, ↑↑ CO, ↓ BP
  • use: chronic HTN, benign prostatic hypertrophy
208
Q

Prednisone

A
  • intermediate acting corticosteroid.
  • can take orally
  • t1/2 = 12-36 hr.
  • adding inhaled corticosteroid decreases the dose
  • use: drug of choice for SLE.
  • start with low dose.
  • increase dose if have: arthritis not responding well to NSAIDs, pleuritis, pericarditis, nephritis.
210
Q

Procainamide

A
  • class IA Na channel blocker
  • ⇒ ↓ conduction velocity
  • convert unidirectional to bidirectional blockade, prolongs refractory period, raises membrane threshold for excitation
  • widened QT interval, prolonged repolarization time
  • use: supraventricular and ventricular arrhythmias
  • toxicity: ↑ ventricular rate, ↓ cardiac contractility, AV block, torsade de pointe, SA arrest, v tach, v fib, lupus erythematous like rxns
210
Q

Probenecid

A
  • blocks URAT at high doses.
  • ⇒ ↑ uric acid secretion
  • use: gout
  • side effects: GI irritation and dermatitis
211
Q

Procaine

A
  • ester local anesthetic
  • weak base, pKa 8.4
  • metabolized by plasma pseudocholinesterase
  • blocks Na channel from inner aspect of membrane.
  • needs to be lipophilic to get to axoplasm.
  • needs to be cationic to get to Na channel.
  • toxicity: CNS = depress inhibitory neurons ⇒ restlessness, tremor, convulsions.
    • cardio = vasodilation, hypotension, ↓ excitability of cardiac muscle, ↓ conduction velocity, ↓ force of contraction.
  • death from respiratory failure
211
Q

Propofol

212
Q

Propranolol

A
  • beta-1 = beta-2 blocker
  • use with diuretics ⇒ synergism ⇒ ↓↓ BP
  • don’t use on ppl with bronchial asthma or COPD
  • use: ischemic heart disease, migraines, HTN
214
Q

Pyridostigmine

A
  • carbamate AChEI
  • oral, IM, IV routes
  • use: myasthenia gravis
215
Q

Quetiapine

A
  • low potency atypical antipsychotic
  • blocks 40-60% D2, and 70-90% 5-HT2A.
  • acute = tranquilizer
  • chronic = antipsychotic after a few wks.
  • good for positive symptoms, a little for negative.
  • use: schizophrenia, psychosis with Parkinson’s disease, psychosis with manic-depressive/schizoaffective disorders or depression.
  • side effects: sedation, cataract and thyroid problems.
216
Q

Quinidine

A
  • class IA Na Channel Blocker, anti-arrhythmic drug.
  • causes ↓ conduction velocity
  • converts unidirectional to bidirectional blockade.
  • prolongs reractory period (K channel block), raises membrane threshold for excitation
  • widened QT interval, prolonged repolarization time.
  • use: supraventricular and ventricular arrhythmias
  • toxicity: ↑ ventricular rate (paradoxical tacycardia), ↓ cardiac contractility, AV block, torsade de pointe, SA arrest, v tach, v fib, GI distress, immune-mediated TTP
  • displaces digoxin ⇒ ↑ free digoxin, ↑ digoxin toxicity, ↓ digoxin Vd
217
Q

Reserpine

A
  • prevents DA entry into vesicle ⇒ ↓ NE
  • **depletes DA in striatum. **
  • use: HTN (with diuretics), Hungtington’s chorea
220
Q

Reteplase

A
  • instead of streptokinase.
  • disolve clots, tissue plasminogen activator.
  • binds Kringle domain, fibrin threads.
  • targets plasminogen, activates to digest fibrin.
  • given IV, t1/2 = 10-30 min. infused slowly
  • use: acute MI (within 6hr onset STEMI), multiple PE, central DVT, acute thrombotic stroke (within 3 hr)
  • do not use with history cerebral hemorrhage or recent head injury
  • pt with chronic HTN ⇒ ↑ risk hemorrhagic stroke
  • toxicity: hemorrhage, cerebral ⇒ death
220
Q

Risperidone

A
  • high potency atypical anti-psychotic
  • blocks 40-60% D2, 70-90 5-HT2A.
  • acute = tranquilizer.
  • chronic = antipsychotic after a few wks.
  • good for positive symptoms, some help with negative.
  • use: schizophrenia, psychosis with manic-drepressive/schizoaffective disorders or depression.
  • side effects: metabolic problems (weight gain)
222
Q

Rivaroxiban

A
  • oral anticoagulant. direct thrombin inhibitor
  • targets factor X and II
  • once a day dosing. t1/2 = 7-11 hr. 2/3 hepatic elimination, 1/3 renal.
  • use: stroke/clot prevention in pt with a. fib. prevent venous thromboembolism in pt for orthopedic surgery.
  • toxicity: hemorrhage, no antidote
222
Q

Rituximab

A
  • biologic DMARD
  • B cell
223
Q

Rivastigmine

A
  • AchE inhibitor
  • ⇒ modest improvement in mild to mod Alzheimer’s.
  • positive effects at low doses
  • use: Alzheimer’s Disease
  • side effects: cholinergic side effects
  • disease continues to progress
224
Q

Rocuronium

A
  • competitive NMJ blockingn agent.
  • large and bulky
  • inhibits amplitude of endplate potentials so propagated action potential can’t develop.
    • histamine release
  • duration: 30-40 mins
  • elimination: 85% bile, 15% renal
  • use: muscle relaxant, anesthetic
  • side effects: autonomic
  • reversed by ACHEI and ↑ extracellular K+
226
Q

Ropinirole

A
  • non-ergot DA receptor agonist
    • preferred over ergots (faster and safer titration)
  • less motor recovery and more side effects than L-DOPA.
  • ↓ risk dyskinesias.
  • use: Parkinson’s Disease, restless-legs syndrome
  • side effects: nausea, vomiting, psychiatric rxns, postural hypotension, sudden onset daytime sleepiness
  • dose related effects eventually outweight therapeutic effects.
227
Q

Rosiglitazone

A
  • TZD. 2nd line add on to metformin
  • activates PPARgamma ⇒ ↑ insulin sensitivity
  • slow onset, euglycemic.
  • ⇒ ↓ fasting glucose, mild ↓ post-prandial
  • redistribute fat from viscera to subQ.
  • ⇒↓ triglycerids, ↑ HDL, ↓ LDL
  • toxicity: weight gain, ↑ risk CHF, ↑ risk bone fractures, ↑ risk hypoglycemia with SU, ↑ risk stroke/MI
228
Q

Salmeterol

A
  • long acting beta agonist.
  • lasts 12 hrs.
  • FEV1 improves in about 30mins
  • use with corticosteroids.
229
Q

Scopolamine

A
  • muscarinic antagonist.
  • atropine with an O
  • **truthe serum **⇒ delirium
  • ↓ nausea and vomiting
  • transdermal
  • crosses BBB ⇒ amnesia = Amazonian zombie
  • use: motion sickness
230
Q

Secobarbital

A
  • barbiturate
  • potentiate GABA at GABA-benzo-chloride channel.
  • short acting
  • metabolized in liver
  • induces CYTP450 metabolism of lipid-soluble drugs (oral BC, carbamazepine, phenytoin, warfarin)
  • chronic use ⇒ tolerance.
  • cross-tolerance btw benzo, barbiturates, ethanol.
  • use: NOT USED PORPHYRIAS
  • side effects: marked sedation, tolerance, respiratory depression
  • withdrawal: anxiety, agitation, life-threatening seizures
    • tx: supportive care, long acting benzo
232
Q

Selegiline

A
  • MAO-B inhibitor.
  • enhances L-DOPA effects.
  • metabolites = aphetamine and methamphetamine ⇒ insomnia and anxiety.
  • use: add on for Parkinson’s Disease
233
Q

Sertraline

A
  • SSRI.
  • selective 5-HT reuptake inhibitor.
  • minimal sedation, weight gain, or autonomic effects.
  • use: depression (1st line), GAD, OCD, phobias, bulimia, pre-menstrual dysphoric disorder, perimenopausal symptoms.
  • side effects: GI discomfort, sexual dysfunction, insomnia, tremor, acute anxiety.
  • discontinuation syndrome if stop suddenly = jittery, anxious, restless.
  • little chance of overdose.
234
Q

Simvastatin

A
  • aka Mevacor/Zocor
  • synthetic derivative of original statin
  • works thru CYP3A4
    • inhibited by grapefruit, erythromycin, ketoconazole
235
Q

Sotol

A
  • beta blocking activity and K channel blockade, Ca channel blocking, and Na channel blocking
  • t1/2 = 20 days
  • prevents re-entry from prolonged refractory period
  • use: a. fib after cardiac surgery; prevent PVC; supraventricular and ventricular arrhythmias
  • toxicity: ↓ cardiac contractility, bradycardia, AV block
236
Q

Spironolactone

A
  • Mineralocorticoid-receptor Antagonist, K+ sparing.
  • t1/2= short, Cannenone (metabolite) has a longer one.
  • competes with DHT for androgen receptor at ↑ concentration ⇒ gynecomastia.
  • targets aldo receptors in collecting duct
  • prevents fibrotic changes in myocardium
  • uses: 1° aldosteronism, 2° aldosteronism, ↓ morbidity and mortality in pts with NYHA class III and IV heart failure, with thiazides for HTN
    • drug of choice for mobilizing edema from hepatic cirrhosis*******
  • side effects: hyperkalemia, gynecomastia, impotence, ↓ libido, hirsutism, deepened voice, menstrual irregularities, diarrhea, gastritis, peptic ulcers, drowsiness, lethargy, ataxia, confusion.
237
Q

Statins

A
  • free acid competes with HMG-CoA reductase and blocks synthesis of cholesterol at rate limiting step
  • ⇒ ↓ intracellular cholesterol in hepatocytes ⇒ ↑ LDLR on cell membrane ⇒ ↓ circulating LDL, ↑ LDL uptake.
  • ↑ exit of cholesterol from bloodstream
  • ⇒ ↑ HMG-CoA levels, ↑ HMG-CoA reductase.
  • good at low doses
  • low bioavailability, stays in liver
  • watch serum aminotransferase activity (AST, ALT)
  • pleiotropic effect: ↑ NO formation in liver, vs high levels ⇒ damage to skeletal muscle
  • toxicity: **rhabdomyolysis **⇒ dark colored urine, ↑ creatinine phosphatase
  • NOT FOR PREGNANT OR NURSING
238
Q

Succinylcholine

A
  • depolarization blocker.
  • flexible and narrow.
  • ⇒ sustained depolarization block of NMJ via nicotinic receptors.
  • muscle fasciculations at onset
  • phase 1 block = with single dose
  • phase 2 block = convert back to competitive block with repeated doses.
  • duration: 5-10 mins, short onset.
  • elimination: plasma pseudocholinesterase
  • use: endotracheal intubation.
  • side effects: activates nicotinic receptors in parasympathetic ganglion (↓ HR, ↓ BP)
  • enhanced by ACHEI and ↑ extracellular K+
239
Q

Sulfasalazine

A
  • non-biologic DMARD
  • combo salicylate and sulfa antibiotic
  • metabolized to sulfapyridine (in RA) and 5-aminosalicylic acid (in IBD)
  • inhibits rheumatoid factor, suppresses T and B cell proliferation, ↓ inflammatory cytokines.
  • takes 1-3 months to show improvement in RA.
  • use: RA that doesn’t respond well to meds, ulcerative colitis
  • side effects: nausea, vomiting, headache, rash.
240
Q

Tamsulosin

A
  • alpha-1 antagonist
  • use: benign prostatic hypertrophy
241
Q

Temazepam

A
  • benzodiazepine.
  • ⇒ liver ⇒ urinary excretion
  • t1/2 is long
  • is a hypnotic (have sedation)
  • use: relief of anxiety, insomnia, sedation and amnesia before procedures, epilepsy and seizure states, muscle relaxation in neuromuscular disorders, ethanol/sedative-hypnotic withdrawal.
243
Q

Terbutaline

A
  • beta-2 agonist
243
Q

Tenecteplase

A
  • plasminogen activator
  • binds Kringle domain to target plasminogen
  • binds fibrin threads
  • ⇒ activation plasminogen to plasmin, digest fibrin.
  • give IV bolus. t1/2 = 10-30 min
  • use: acute MI (within 6hr onset STEMI), multiple PE, central DVT, acute thrombotic stroke (within 3 hr onset)
  • don’t use if history of cerebral hemorrhage or recent head injury
  • pt with chronic HTN ⇒ ↑ risk hemorrhagic stroke
  • toxicity: hemorrhage, cerebral ⇒ death
245
Q

Thiopental

A
  • barbiturate
  • potentiate GABA at GABA-benzo-chloride channel.
  • short acting
  • metabolized in liver
  • induces CYTP450 metabolism of lipid-soluble drugs (oral BC, carbamazepine, phenytoin, warfarin)
  • chronic use ⇒ tolerance.
  • cross-tolerance btw benzo, barbiturates, ethanol.
  • causes redistribution
  • use: induction of amnesia
    • NOT USED PORPHYRIAS
  • side effects: marked sedation, tolerance, respiratory depression
  • withdrawal: anxiety, agitation, life-threatening seizures
    • tx: supportive care, long acting benzo
245
Q

Tetracaine

A
  • ester local anesthetic
  • metabolized by plasma pseudocholinesterase.
  • blocks Na channel from inside axoplasm.
  • toxicity: CNS = depress inhibitory neurons ⇒ restlessness, tremor, convulsions.
    • cardio = vasodilation, hypotension, ↓ excitability of cardiac muscle, ↓ conduction velocity, ↓ force of contraction
  • death from respiratory failure
247
Q

Tiagabine

A
  • inhibits GAT-1, a GABA transporter.
  • use: simple partial seizures, complex partial seizures.
247
Q

Thioridazine

A
  • low potency typical antipsychotic
  • blocks D2, M1, H1, and alpha-1.
  • takes a few weeks to take effect
  • helps with positive symptoms.
  • use: schizophrenia
  • _side effect_s: block M1 ⇒ ↑ body temp, cognitive impairment, constipation, urinary retention, closed-angle glaucoma, ↓ seizure threshold, cardiotoxicity (QT prolongation is really bad).
    • blocks H1 ⇒ weight gain, sedation, ↑ risk type 2 diabetes.
    • block alpha-1 ⇒ orthostatic hypontension.
    • block D2 ⇒ ↑ prolactin ⇒ galactorrhea, amenorrhea, infertility.
    • tardive dyskinesia, parkinsonism, irreversible retinal pigmentation.
    • can cause fatal arrhythmias with overdose or with TCAs.
249
Q

Ticagrelor

A
  • platelet inhibitor.
  • nucleoside analog, acts as negative allosteric modulator
  • inhibits ADP receptor contributes to platelet activation (GPCR:P2Y12) competitive inhibitor
  • major metabolite is also active
  • give 2x a day, t1/2 = 7hr
  • use: prevent thrombosis after MI, vascular events, before/after PCI or CABG, a. fib, or unstable angina.
  • not for stroke or TIA.
  • toxicity: hemorrhage, skin rashes, GI problems
250
Q

Tiludronate

A
  • bisphosphonate, oral.
251
Q

Timolol

A
  • beta-1 = beta-2 antagonist
  • ⇒ ↓ intraocular pressure
  • use: glaucoma, ischemic heart disease
252
Q

Topiramate

A
  • prolongs inactivation of Na channel.
  • use: simple partial seizures, complex partial seizures, tonic-clonic seizures.
253
Q

Timolol

A
  • beta-1 = beta-2 antagonist
  • ⇒ ↓ intraocular pressure
  • use: glaucoma, ischemic heart disease
254
Q

Tiotropium

A
  • long acting anticholinergic
  • high affinity for M1 and M3.
  • onset 30 min, peak 3hr, t1/2 = 35hr.
  • efficacy gradually increases.
  • ⇒ pupillary dilation
  • ⇒ ↓ incidence COPD exacerbations
  • use: asthma
255
Q

Tirofiban

A
  • synthetic peptide fragment containing RGD motif, blocks GpIIb/IIIa receptors.
  • inhibits fibrinogen-dependent aggregation of activated platelets.
  • use: clot prevention during PCI and prevent restenosis after PCI
  • toxicity: bleeding
257
Q

Tramadol

A
  • weak mu agonist, inhibits reuptake of NE and 5-HT.
  • analgesia not fully blocked by naloxone.
  • low abuse potential
  • use: mild to mod pain, chronic pain, MI, acute dyspnea from heart failure, analgesia, anesthesia
  • side effects: modest respiratory depression, ↓ seizure threshold
257
Q

Triamterene

A
  • K sparing diuretic
258
Q

Tranylcypromine

A
  • MAOI
    • irreversibly inhibit MAO-A and MAO-B.
  • use: depression when can’t use other drugs from toxicity.
  • side effects: weight gain, postural hypertension, sexual dysfunction, altered sleep.
  • hypertensive crisis: if taken with foods with tyramine or OTC decongestants (phenylephrine, pseudoephedrine).
  • serotonin syndrome = rigidity, hyperthermia, altered mental status, cardiovascular collapse)
    • if taken with SSRIs, meperidine, or dextromethorphan.
  • overdose: CNS intoxication (agitation, delirium, seizures, coma). can be fatal.
259
Q

Trazodone

A
  • antidepressant
  • blocks 5-HT2A.
  • H1 blockade.
  • block alpha-1 ⇒ reduce nightmares in PTSD.
  • active metabolite = m-chlorophenylpiperazine.
  • use: depression, sleep aide.
  • side effect: sedation, priapism
260
Q

Triamcinolone

A
  • inhaled corticosteroid
260
Q

Tubocurarine

A
  • nicotinic antagonist
  • non-depolarizing neuromuscular blocking agent
  • reversed by AChE
261
Q

UFH

A
  • unfractionated heparin.
  • anticoag drug, inhibits activated coag factors (thrombin and Factor Xa)
  • give IV or s.c. t1/2 = 90 min
  • binds ATIII with high affinity, inhibits factors Xa, VIIa, IXa.
  • 2 binding sites: ATIII and thrombin
  • does not cross BBB, safe during pregnancy
  • cleared by reticuloendothelial system
  • monitor aPTT to ensure dosing
  • use: acute/chronic tx of arterial/venous thrombosis, clot prevention
  • toxicity: hemorrhage, osteoporosis (chronic), HIT
262
Q

Valproate

A
  • aka sodium valproate, valproic acid, Depakote
  • prolongs inactivation of Na channel.
  • inhibits GABA-T and succinic semi-aldehyde dehydrogenase.
  • closes T type Ca channels
  • levels reduced by carbamazepine
  • use: absence seizures, partial seizures, clonic-tonic seizures, migraine prophylaxis, manic phase of bipolar disorder.
  • side effects: nausea, dizziness, sedation, vomiting, hepatotoxicity
262
Q

Triamterene

A
  • K+ sparing diuretic
  • blocks ENaC in principal cell ⇒ blocks effects of aldosterone
  • promotes acidosis, spares (H+), makes less negative lumen for K+ sparing.
  • uses; Liddle’s syndrome (HTN, ↓ renin, metabolic alkalosis, hypokalemia, normal aldosterone), Lithium induced nephrogenic diabetes insipidus, with thiazides for HTN and edema.
263
Q

Vancomycin

A
  • 2nd line treatment for C diff. cidal. give IV
  • inhibits cell wall synthesis.
  • renal excretion
  • mechanism: interferes with cleavage of peptidoglycan precursor peptide from membrane phospholipid. binds to D-ala D-ala
  • use: strep, staph, enterococci, MRSA, C diff, diptheria, gram (+)
    • serous endocarditis or staph/strep not responding
  • toxicity: ototoxicity, nephrotoxicity, Redneck syndrome: stimulates mast cells ⇒ histamine. slow down infusion rate.
263
Q

Triazolam

A
  • benzodiazepine with triazole group
  • extremely rapid acting, short duration
  • metabolite: alpha-hydroxy metabolites ⇒ liver ⇒ urinary excretion
  • t1/2 = 3-5 hrs.
  • is a hypnotic (sedation)
  • use: relief of anxiety, insomnia, sedation and amnesia before procedures, epilepsy and seizure states, muscle relaxation in neuromuscular disorders, ethanol/sedative-hypnotic withdrawal.
  • side effects: rebound anxiety, next day amnesia, confusion.
264
Q

Tropicamide

A
  • tertiary amine
  • mydriatic and cycloplegic drug
265
Q

Vecuronium

A
  • competitive NMJ blockingn agent.
  • large and bulky
  • inhibits amplitude of endplate potentials so propagated action potential can’t develop.
    • histamine release
  • duration: 30-40 mins
  • elimination: 85% bile, 15% renal
  • use: muscle relaxant, anesthetic
  • side effects: autonomic
  • reversed by ACHEI and ↑ extracellular K+
270
Q

Venlafaxine

A
  • SNRI, short t1/2.
  • blocks NE and 5-HT reuptake.
  • use: depression, chronic pain disorders.
  • side effects: 6-13% develop HTN, GI discomfort, sexual dysfunction, insomnia, tremor, acute anxiety.
  • can get 5-HT discontinuation syndrome.
271
Q

Verapamil

A
  • non-DHP CCB (phenyalkylamine). powerful dilator.
  • metabolized by CYP3A4
  • affects inner part of Ca channel, the gating mechanism
  • erratic absorption, low bioavailability
  • ⇒ ↓ HR and contractility ⇒ ↓ SA node rate, ↑ refractory period, ↑ PR interval
  • use: migraines, angina, HTN, arrhythmias
  • side effects: peripheral edema, hypotension, tachycardia, palpitations, flushing, headache, dizziness, nausea, ↑ digoxin levels
  • ↑ levels when taken with grapefruit, ketoconazole, erythromycin
  • rifampin ⇒ ↓ levels
  • use with beta blocker ⇒ severe bradycardia, AV blocks, reverse by atropine or Ca gluconate
  • inhibits P-glycoprotein
272
Q

Vigabratrin

A
  • inhibits GABA-T, a GABA transaminase ⇒ ↑ GABA.
273
Q

Warfarin

A
  • aka Coumadin
  • indirectly inhibits throbin, blocks clotting factors by competing with vit K (inhibits vit K epoxide reductase VKOR ⇒ inhibit II, IV, V, IX, X, protein C and S)
  • take orally, 100% bioavailable, lipophilic
  • t1/2 = 36-48 hr. 160hr to steady state.
  • dose based on CYP450 levels, keep INR 2-3.
  • NOT USED DURING PREGNANCY, impeded bone development
  • use: tx arterial/venous thrombosis, venous thromboembolism in pt with a fib, artificial valves, pt with antiphospholipid syndrome, orthopedic surgery, prevent MI/stroke in high risk pt.
  • toxicity: hemorrhage, skin necrosis, birth defects, osteoporosis (chronic use)
  • drug interactions: ↑ anticoag from ↓ metabolism by amiodarone, fluoxetine, cimetidine, metronidazole
    • **antibiotics **⇒ ↓ effect from ↑ warf metabolism
    • **cholestyramine **⇒ ↓ anti-coag from ↓ warf GI absorption
    • NSAID, heparin ⇒ ↑ anti-coag from enhancement
274
Q

Zafirlukast

A
  • LTD4 and LTE4 receptor antagonist.
  • use: asthma
275
Q

Zaleplon

A
  • aka Sonata
  • selective benzodiazepine receptor agonist.
  • t1/2 = 1-2 hours.
  • metabolized via aldehyde dehydrogenase.
  • binds BDZ1 receptors.
  • shortens sleep latency and ↑ total sleep
  • tolerance is rare.
  • use: hypnotic (sedation), prevent jet lag
  • side effects: rebound insomnia when stoping.
276
Q

Zileuton

A
  • 5-lipoxygenase inhibitor.
  • use: asthma
  • liver function tests needed.
277
Q

Ziprasidone

A
  • medium potency atypical antipsychotic
  • blocks 40-60% D2, and 70-90% 5-HT2A.
    • some 5-HT1A agonist activity = antidepressant.
  • acute = tranquilizer
  • chronic = antipsychotic after a few wks.
  • good for positive symptoms, a little for negative.
  • use: schizophrenia, psychosis with manic-depressive/schizoaffective disorders or depression.
  • side effects: sedation, QT prolongation.
278
Q

Zolendronate

A
  • bisphosphonate, parenteral
  • can ⇒ acute kidney failure
279
Q

Zolpidem

A
  • aka Ambien.
  • selective benzodiazepine receptor agonist.
  • t1/2 = 1.5-3.5 hours.
  • no active metabolites.
  • bind to BDZ1 receptors.
  • shorten sleep latency and ↑ total sleep
  • tolerance is rare.
  • use: hypnotics, prevent jet lag.
  • side effects: rebound insomnia when stopping, some sleepwalking.

Pharmacology (6 decks)

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