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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
**Aspart**
* rapid acting insulin
22
**Aspirin**
* **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
24
**Atenolol**
* **beta-1 antagonist** beta-1 \>\>\> beta-2 * at high doses blocks beta-2
24
**Atorvastatin**
* aka Lipitor * **statin**, potent * 10mg ⇒ **↓ LDL (35%)**. 20mg ⇒ 45%, 40mg ↑ toxicity * works thru **CYP3A4** * inhibited by grapefruit, erythromycin, ketoconazole
25
**Atracurium**
* **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+**
26
**Atropine**
* **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**.
27
**Azathiprine**
* **anti-metabolite**, looks like purine. * blocks DNA synthesis ⇒ **blocks proliferating T cells** * _use_: **immunosuppressive therapy** * _side effect_: **bone marrow suppression/toxicity**.
28
**Beclomethasone**
* inhaled corticosteroid
29
**Benztropine**
* **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)
31
**Beta Blockers arrhythmias**
* 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**
31
**Beta Blockers**
* **⇒ ↓ 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.
32
**Betaxolol**
* beta-1 \>\>\> beta-2 antagonist
33
**Bethanechol**
* 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)
33
**Brimonide**
* alpha-2 agonist
35
**Bromocriptine**
* **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.
36
**Bupivacaine**
* **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.
37
**Buspirone**
* 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)
38
**Butorphanol**
* 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**
39
**Ca Channel Blockers (CCB)**
* _use_: supraventricular tachycardia
40
**Carbachol**
* **direct acting agonist** * **good muscarinic and nicotinic activity** * not susceptible to AChE * _use_: **glaucoma**
40
**Captropril**
* **alkyl ACEI**. * short acting, given 2-3 times per day
42
**Carbidopa**
* **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.
42
**Carbamazepine**
* 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**
44
**Carteolol**
* beta-1 = beta-2 antagonist
45
**Carvedilol**
* **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**
45
**CCB**
* 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**
46
**CCB arrhythmias**
* ⇒** ↓ 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
47
**Celecoxib**
* **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**.
48
**Cervistatin**
* statin. * too toxic, not on market * 200x Fluvastatin
49
**Chlordiazepoxide**
* **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.
50
**Chlorpromazine**
* **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**.
51
**Cholestyramine**
* **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**
52
**Cimetidine**
* CYP inhibitor * use: stomach ulcer
52
**Cilostazol**
* **PDE-3 inhibitor** ⇒ ↑ cAMP, vasodilation, **inhibits platelet function.** * _use_: **intermittent claudication**
53
**Clofibrate**
* **fibric acid derivative** * ⇒ ↓ triglyceride levels in blood, ↑ activity of LPL (TG lipase)
53
**Citalopram**
* **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.
54
**Clomipramine**
* **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
55
**Clonidine**
* **alpha-2 agonist** * ⇒ **↓ synaptic NE**
56
**Clopidogrel**
* 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**
57
**Clozapine**
* **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.**
59
**Cocaine**
* **inhibits DA reuptake** in CNS. * rapidly penetrates BBB ⇒ **elation and euphoria**. * major drug of abuse.
60
**Codeine**
* 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**.
61
**Colchicine**
* **inhibits granulocyte migration and phagocytosis**. * acts in 12-24 hrs. * _use_: **gout**. * _side effects_: **nausea, vomiting, abd pain, diarrhea** * _intoxication _⇒ **bloody diarrhea, shock, hematuria**
62
**Colestipol**
* **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**
62
**Colesevelam**
* **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**
62
**Coxibs**
* NSAID. inhibits COX2. * Celecoxib (Celebrex) and Rofecoxib
62
**Cyclophosphamide**
* non-biologic DMARD * _use_: SLE
63
**Dantrolene**
* direct acting * **inhibits calcium release from sarcoplasmic reticulum** * _use_: **spastic condictions** * _side effects_: **hepatotoxicity**
64
**Darifenacin**
* selective inhibitor for M3
66
**Desipramine**
* **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
67
**Detemir**
* **long acting insulin**. s.c. * onset 1-5 hr, no peak, lasts 12-24 hr. * _use_: **type 1 DM**
68
**Dexamethasone**
* **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**.
70
**Dextromethorphan**
* _use_: **cough suppression**.
71
**Diclofenac**
* **COX1 and COX2 inhibitor**. * analgesic * ⇒ **↓ arachidonic acid release in leukocytes**. * **high concentration in synovial fluid**. * _use_: **RA**.
71
**Diazepam**
* 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.
73
**Digoxin**
* **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
73
**Diltiazem**
* 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)
74
**Diphenhydramine**
* **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**)
75
**Dipyridamole**
* ⇒ **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)
76
**Disopyramide**
* **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**
77
**Dobutamine**
* **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**
77
**Donepezil**
* **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
78
**Doxazosin**
* **alpha1 antagonist** * alpha1\>\>\>\>alpha2
78
**Dopamine**
* **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**
79
**Duloxetine**
* **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.
81
**Echothiophate**
* **irreversible indirect acting organophosphate AChEI** * itraocular route * _use_: **glaucoma**
82
**Edrophonium**
* **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**
83
**Enalapril**
* **alkyl ACEI**. * short acting * give 1-2 times per day
84
**Ephedrine**
* can cross BBB
85
**Epinephrine**
* **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
85
**Eptifabatide**
* **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**
86
**Escitalopram**
* 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.
87
**Esmolol**
* aka Breviboc * **beta-1 antagonist**. * short duration = 10 min * popular in **surgical procedures**
88
**Esomeprazole**
* proton pump inhibitor. * inhibits CYP2C19
89
**Eszopiclone**
* 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.
90
**Etanercept**
* 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.
91
**Ethacrynic Acid**
* **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**
92
**Ethosuximide**
* **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.**
94
**Exenatide**
* **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**.
95
**Exetimibe**
* **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
96
**Febuxostat**
* **non-competitive inhibitor Xanthine oxidase**. * **irreversibly** inhibits. * ⇒ **↑ excretion uric acid**. * _use_: **gout**
97
**Fenofibrate**
* **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)
98
**Fentanyl**
* 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**
99
**Flecainide**
* **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.
101
**Fludrocortisone**
* **short-acting mineralcorticoid**. * t1/2 = 8-12 hr. * _use_: **acute adrenocortical insufficiency, Addison's disease.**
101
**Fluoxetine**
* **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.
102
**Fluphenazine**
* **high potency typical antipsychotic**. * blocks **D2** * use low doses, **milder sedation** * _use_: **schizophrenia** * _side effects_: **tardive dyskinesia, akathisia, parkonsonism, acute dystonia, hyperprolactinemia**.
103
**Fluticasone**
* inhaled corticosteroid
104
**Fluvastatin**
* statin
105
**Formoterol**
* **long acting beta agonist**. * **↑ risk asthma related death**. * use with corticosteroids.
106
**Furosemide**
* **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
**Gabapentin**
* 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
**Galantamine**
* **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
**Glargine**
* **long acting insulin**. s.c. * onset 1-2 hr, no peak, lasts \>24hrs. * _use_: **type 1 DM**
110
**Glimepiride**
* **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
**Glipizide**
* **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
**Glucocorticoids**
* CYP3A4 inducer * use: osteoarthritis, RA, SLE.
114
**Glulisine**
* rapid acting insulin
115
**Glycopyrrolate**
* quaternary amine. * _use_: **GI hypermotility**
115
**Glyburide**
* **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_: t**ype I DM, pregnancy, stress, surgery, infection, renal/liver impairment**. * _side effects_: **hypoglycemia, weight gain, nausea, vomiting, GI discomfort.**
116
**Haloperidol**
* **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
**Halothane**
* halogenated inhaled anesthetic
119
**Homatropine**
* **muscarinic antagonist**. * atropine with -OH
120
**Hydralazine**
* 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
**Hydrochlorothiazide**
* **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
**Ibuprofen**
* 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
**Ibandronate**
* **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
**Imipramine**
* **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
**Indomethacin**
* **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
**Infliximab**
* 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
**Insulin**
* **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
**Ipratropium**
* **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
**Isocarboxazid**
* **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
**Isoproterenol**
* **beta-1 = beta-2 agonist** * beta-1 ⇒ ↑ HR ⇒ ↑ CO ⇒ **↑ BPsys** * beta-2 ⇒ ↓ TPR ⇒ **↓ BPdia** * for beta-2, iso\>epi\>\>NE
130
**Isosorbide**
* **osmotic diuretic** * orally active
132
**Isosorbide Dinitrate**
* **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
**Ketorolac**
* **analgesic** * replaces morphine after surgery
133
**Ketoprofen**
* 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
**L-DOPA**
* converted by DOPA-decarboxylase to DA. * ⇒ **↑ DA release by surviving neuron**s. * 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
**Labetolol**
* **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
**Lamotrigine**
* prolongs **inactivation of Na channel**. * _use_: **simple partial seizures, complex partial seizures, tonic-clonic seizures, acute manic episodes and prophylaxis.**
138
**Latanoprost**
* **PFG2 analog**. * _use_: **glaucoma, ocular HTN**
139
**Lidocaine**
* **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
**Levothyroxine**
* **T4**. * 80% bioavailability * t1/2 = 7 days * start immediately * _use_: **hypothyroidism** * in elderly, **if have angina or cardiac arrhythmia then ↓ dose.**
141
**Liraglutide**
* **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
**Lisinopril**
* **ACEI** * long acting * 1-2 times per day
143
**Lispro**
* **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
**Lithium Carbonate**
* **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
**LMW Heparin**
* 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
**Loperamide**
* 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
**Lorazepam**
* **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
**Lovastatin**
* 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
**Melocicam**
* COX2 inhibitor.
149
**Mannitol**
* **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
**Memantine**
* **NMDA receptor, negative allosteric modulator** * _use_: **mod to severe Alzheimer's Disease** * small benefit * disease still progresses
151
**Meperidine**
* 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
**Mepivacaine**
* **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
**Metformin**
* **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
**Methacholine**
* **good muscarinic activity** * no nicotinic activity * **slightly susceptible to AChE** * _use_: **glaucoma**
156
**Methimazole**
* **inhibits TPO**, antithyroid drug * use after **1st trimester** in pregnancy * less hepatotoxicity * _use_: **hyperthyroidism** * _side effects_: **rash, nausea, GI discomfort, agranulocytosis**
156
**Methadone**
* 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
**Methotrexate**
* **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
**Metoclopramide**
* promotes stomach emptying
160
**Metoprolol**
* **beta-1 antagonist ** * ↓ renin release, ↓ HR, ↓ myocardial O2 consumption, ↓ downregulation of beta receptors
161
**Mevostatin**
* 1st statin discovered. * from mold
162
**Midazolam**
* use: conscious sedation, pre-medication for monitored anesthesia
163
**Miglitol**
* **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
**Mirtazapine**
* **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
**Misoprostol**
* **PGE1 analog** * _use_: **early abortion**, tx of **miscarriage**, prevent **NSAID-induced peptic ulcer**.
166
**Mivacurium**
* **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
**Montelukast**
* **leukotriene receptor blocker** * _use_: **asthma, allergic rhinitis**
168
**Morphine**
* 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
**Na Nitroprusside**
* cardiac unloading agent. * ⇒ ↑ sympathetic outlfow * ⇒ **NO spontaneously.** * dilates arterioles ⇒ **↓↓ LV EDP, ↑↑ CO, ↓ BP**
170
**Nabumetone**
* NSAID. inhibits COX2.
171
**Naproxen**
* 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
**Neostigmine**
* **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
**Nifedipine**
* **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
**Niacin**
* **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
**Nimodipine**
* **CCB**. * given IV * lipophilic, **crosses BBB** * _use_: **SAH** from burst cerebral aneurysm * ⇒ ↓ neurological deficit
176
**Nitroglycerin**
* 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
**Norepinephrine**
* **alpha-1 alpha-2 beta-1 agonist** * alpha-1\>beta-1 effects ⇒ ↓ HR, ↑ BP * sympathetic withdrawal thru baroreceptors * **NE ⇒ ↑ TPR, ↑ BP, ↓ HR**
178
**NPH** **NPL** **NPA**
* **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
**Nortriptyline**
* **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
**Ocreotide**
* **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
**Olanzapine**
* **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
**Omalizumab**
* **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
**Omeprazole**
* proton pump inhibitor * inhibits CYP2C19
183
**Ondansetron**
* 5-HT3 antagonist ⇒ antiemetic
184
**Opioid Overdose**
* **coma** * **pinpoint pupils** * **depressed respiration**
186
**Oxybutynin**
* **M antagonist = M3** * prevents **urge incontinence** for hyperactive bladder
186
**Oxazepam**
* **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
**Oxytocin**
* **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
**Pancuronium**
* **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
**Paroxetine**
* **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
**Pentobarbital**
* **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
**Phenelzine**
* **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
**Phenobarbital**
* CYP2C9 inducer
196
**Phenoxybenzamine**
* **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
**Phentolamine**
* **alpha-1 = alpha-2 antagonist** * **↑ sympathetic outflow** * dilates arterioles and veins ⇒** ↓↓ LV EDP, ↑↑ CO, ↓BP**
197
**Phenylephrine**
* **alpha-1 agonist** * ⇒ ↑ TPR ⇒ **↑ BP, ↓ HR** * not recognized by COMT
199
**Physostigmine**
* **irreversible indirect acting carbamide AChEI** * works at anionic and esteratic sites * intraocular, IM, IV routes. * long lasting * **crosses BBB** * _use_: **glaucoma, atropine intoxication**
199
**Phenytoin**
* **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
**Pilocarpine**
* **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
**Pioglitazone**
* **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
**Pramlintide**
* ⇒ **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
**Pramipexole**
* **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
**Prasugrel**
* **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
**Prazosin**
* **alpha-1 antagonist** * ⇒ ↑ sympathetic flow * dilates arterioles ⇒ **↓↓ LV EDP, ↑↑ CO, ↓ BP** * _use_: **chronic HTN, benign prostatic hypertrophy**
208
**Prednisone**
* **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
**Procainamide**
* **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
**Probenecid**
* **blocks URAT** at high doses. * ⇒ **↑ uric acid secretion** * _use_: **gout** * _side effects_: **GI irritation and dermatitis**
211
**Procaine**
* **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
**Propofol**
212
**Propranolol**
* **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
**Pyridostigmine**
* **carbamate AChEI** * oral, IM, IV routes * _use_: **myasthenia gravis**
215
**Quetiapine**
* **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
**Quinidine**
* **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
**Reserpine**
* **prevents DA entry into vesicle ⇒ ↓ NE** * **depletes DA in striatum. ** * _use_: **HTN** (with diuretics), **Hungtington's chorea**
220
**Reteplase**
* 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
**Risperidone**
* **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
**Rivaroxiban**
* 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
**Rituximab**
* biologic DMARD * B cell
223
**Rivastigmine**
* **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
**Rocuronium**
* **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
**Ropinirole**
* **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
**Rosiglitazone**
* **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
**Salmeterol**
* **long acting beta agonist**. * lasts 12 hrs. * **FEV1 improves in about 30mins** * use **with corticosteroids**.
229
**Scopolamine**
* **muscarinic antagonist**. * atropine with an O * **truthe serum **⇒ delirium * ↓ nausea and vomiting * transdermal * **crosses BBB** ⇒ amnesia = Amazonian zombie * _use_: **motion sickness**
230
**Secobarbital**
* **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
**Selegiline**
* **MAO-B inhibitor**. * **enhances L-DOPA effects**. * metabolites = aphetamine and methamphetamine ⇒ **insomnia and anxiety.** * _use_: add on for **Parkinson's Disease**
233
**Sertraline**
* **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
**Simvastatin**
* aka Mevacor/Zocor * **synthetic derivative of original statin** * works thru **CYP3A4** * inhibited by grapefruit, erythromycin, ketoconazole
235
**Sotol**
* **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
**Spironolactone**
* **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
**Statins**
* **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
**Succinylcholine**
* **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
**Sulfasalazine**
* **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
**Tamsulosin**
* **alpha-1 antagonist** * _use_: **benign prostatic hypertrophy**
241
**Temazepam**
* **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
**Terbutaline**
* beta-2 agonist
243
**Tenecteplase**
* **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
**Thiopental**
* **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
**Tetracaine**
* **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
**Tiagabine**
* **inhibits GAT-1**, a GABA transporter. * _use_: **simple partial seizures, complex partial seizures**.
247
**Thioridazine**
* **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.**
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**Ticagrelor**
* **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**
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**Tiludronate**
* bisphosphonate, oral.
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**Timolol**
* **beta-1 = beta-2 antagonist** * ⇒ ↓ intraocular pressure * _use_: **glaucoma, ischemic heart disease**
252
**Topiramate**
* prolongs **inactivation of Na channel**. * _use_: **simple partial seizures, complex partial seizures, tonic-clonic seizures**.
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**Timolol**
* **beta-1 = beta-2 antagonist** * ⇒ ↓ intraocular pressure * _use_: **glaucoma, ischemic heart disease**
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**Tiotropium**
* **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**
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**Tirofiban**
* **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**
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**Tramadol**
* **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**
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**Triamterene**
* K sparing diuretic
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**Tranylcypromine**
* **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
**Trazodone**
* **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**
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**Triamcinolone**
* inhaled corticosteroid
260
**Tubocurarine**
* nicotinic antagonist * **non-depolarizing neuromuscular blocking agent** * **reversed by AChE**
261
**UFH**
* 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**
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**Valproate**
* 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**
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**Triamterene**
* **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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**Vancomycin**
* **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.
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**Triazolam**
* **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**.
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**Tropicamide**
* tertiary amine * **mydriatic and cycloplegic drug**
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**Vecuronium**
* **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
**Venlafaxine**
* **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
**Verapamil**
* **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**
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**Vigabratrin**
* **inhibits GABA-T**, a GABA transaminase ⇒ ↑ GABA.
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**Warfarin**
* 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**
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**Zafirlukast**
* **LTD4 and LTE4 receptor antagonist**. * _use_: **asthma**
275
**Zaleplon**
* 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.
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**Zileuton**
* **5-lipoxygenase inhibitor**. * _use_: **asthma** * liver function tests needed.
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**Ziprasidone**
* **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**.
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**Zolendronate**
* bisphosphonate, parenteral * can ⇒ acute kidney failure
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**Zolpidem**
* 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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