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Pharmacology Final > Drug Classes&Names > Flashcards

Drug Classes&Names Flashcards

1
Q

Bronchodilators (COPD and Asthma Treatment)

A
  1. beta2 selective agonists
  2. Leukotriene Inhibitors
  3. Methylxanthines
  4. Muscarinic Antagonists
  5. Antihistamines (mast cell stabilizers)
  6. Anti-IgE Ab (Omalizumab)
  7. Corticosteroids
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2
Q

Beta2 selective agonists

A

-rol suffix
1. Albuterol (Salbutamol)
2. Terbutaline
3. Fenoterol
4. Salmeterol
5. Formoterol
MOA: Bind β2 Rs on Bronchial tree-> Gs couples Increased cAMP-> Smooth m. relaxation -> Bronchodilation

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3
Q

Muscarinic antagonists (for bronchodilation)

A
  1. Ipratropium
  2. Tiotropiuum
    MOA: M3R inhibitor (Gq-coupled)-> Prevent bronchoconstriction by vagal discharge
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4
Q

Methylxanthines

A

Theophylline

MOA: PDE Inhibition-> Increased cAMP-> Bronchodilation, decreased inflammation. CYP450!!

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5
Q

Corticosteroids (for bronchodilation)

A
  1. Budesonide, Dexamethasone
  2. Prednisolone
    MOA: Inhibit PLA2 -> Decrease COX-> Less inflammatory mediators
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6
Q

Leukotriene antagonists

A

Montelukast

MOA: Inhibit LT synthesis/action-> Less inflammation + less bronchoconstriction

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7
Q

Antihistamines (Mast cell stabilizers - bronchodilation)

A

Cromolyn (not in excel sheet but important)

MOA: Prevent degranulation of mast cells

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8
Q

Anti-IgE antibody

A

Omalizumab

MOA: Bind Fc portion of IgE Abs -> cannot bind to mast cells -> no inflammatory response

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9
Q

Cough medication

A
  1. Antitussive agents (non-productive cough)

2. Muco-active (productive cough) - Expectorants& Mucolytics

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10
Q

Antitussive agents

A
  1. Codeine (Opioid)
    MOA: μ-Receptor agonist. Suppress cough reflex
  2. Butamirate (Non-opioid) & Prenoxidiazine
    MOA: Centrally acting - Suppress cough reflex. Peripheral -> Bronchodilation, suppress inflammation
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11
Q

Muco-active Drugs

A
  1. Mucolytics:
    Bromhexine (MOA: Increase serous fluid production)
    Acetylcysteine (MOA: Decrease disulfide bonds in mucus, decrease viscosity)
  2. Expectorants
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12
Q

Peripheral Vascular Disease drugs

A
  1. General - Statins, Aspirin/Clopidogrel, Anti-HTN, ACE Inhibitors/ARBs (1st line of treatment)
  2. Cilostazol (PDE-3 Inhibitor, Vasodilation)
  3. Pentoxifyllin (Reduce blood viscosity)
  4. Vinpocetin (Inhibit Na &Ca channels, increase cerebral perfusion)
  5. Nicergoline (α1 antagonist, Cholinergic function, decrease platelet aggregation, increase metabolism, neurotrophic & antioxidant)
  6. Ca-Dobesilate (Reduce microvascular permeability)
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13
Q

Migraine Treatment

A
  1. Acute Attack Therapy

2. Prophylactic Therapy (>4 attacks/month, severe attacks, >72hrs)

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14
Q

Acute Migraine Attack Therapy

A
  1. Non-specific:
    Acetaminophen, Aspirin, caffeine, NSAIDs, Metoclopramide, Droperidol
  2. Migraine specific:
    Sumatriptan (MOA: 5-HT1D/1B agonist, Vasoconstriction, Decreased NP release, brainstem to inhibit pain pathway)
    Ergotamine (MOA: Partial 5-HT2& αAR agonist)
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15
Q

Migraine Prophylactic Therapy

A
  1. Galcanezumab (MOA: CGRP antagonist-Vasoconstriction. Minoclonal Ab)
  2. Cinnarizine (MOA: Anti-histamine, Ca-channel blocker)
  3. Propanolol (MOA: β-non selective antagonist)
  4. Verapamil (MOA: Ca-ch. blocker, Non-DHIP)
  5. Carbamazepin (MOA: Inhibit voltage-gated Na ch, less glutamate release)
  6. Valproic acid (MOA: Inhibit high-freq. firing, Inhibitory actions of GABA)
  7. Imipramine (MOA: inhibit 5-HT &NE reupate - Tricylic antidepressant) CYP450!!
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16
Q

ACE Inhibitors

A

-pril suffix
1. Captopril
2. Enalapril (1×5-20mg in hypertension)
3. Perindopril
4. Ramipril
MOA: Inhibit ACE, so low AngTensin II and Aldosterone levels, Increase endogenous vasodilators (bradykinin)
First line treatment for Heart Failure

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17
Q

ARBs

A

-sartan suffix
1. Losartan
2. Valsartan (1×80-320mg in hypertension)
3. Irbesartan
MOA: Comp inhibitors of AT1R-> Prevent vasoconstriction, low aldosterone, low ADH, decrease SNS stimulation, prevent cardiac hypertrophy

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18
Q

Heart Failure Treatment (Decrease load on heart)

A
  1. ACE Inhibitors/ ARBs
  2. Diuretics (Thiazides, Loop, K+ Sparing agents)
  3. Beta blockers
  4. Vasodilators (isosorbide dinitrate, hydralazine,NO)
  5. PDE Inhibitors (Milrinone, Theophylline) - For AHF
  6. Neprilysin inhibitors (Sacubitril) - For CHF
  7. Ca-sensitizing agents (Levosimendan) - For AHF
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19
Q

Heart Failure Treatment (Positive Inotropic agents)

A

Digoxin (maintenance dose 1×0,25mg)

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20
Q

Acute Heart Failure Treatment

A
  • beta agonists (Dobutamine & Dopamine)
  • diuretics (MRAs, Acetazolamide)
  • vasodilators (Isoborbide dinitrate, hydralazine)
  • PDE Inhibitors (Milrinone, Theophylline)
  • ACE Inh/ARBs
  • Calcium sensitizers (levosimendan)
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21
Q

Chronic Heart Failure Treatment

A
  • Digoxin
  • Diuretics
  • Beta blockers
  • ACE-Inhibitors/ARBs
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22
Q

Digoxin MOA

A
  • Inhibit cardiac Na/K ATPase, Increase Intracellular Na+, Alter driving force for Na/Ca exchanger -> Increased Intracellular Ca -> Increase Ca-release from SR -> Increased actin-myosin interaction -> Increased Contractile force
  • Inhibit neuronal Na/K ATPase, Increase Vagal activity-> Negative chronotropy
  • Decrease AV conduction -> negative dromotropy
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23
Q

Types of Diuretics

A
  1. Carbonic anhydrase inhibitors
  2. Osmotic diuretics (aquaretics)
  3. Loop Diuretics
  4. Thiazides
  5. K+ - Sparing
  6. SGLT-2 antagonists (not used as a diuretic but will increase urine volume)
  7. Drugs affecting ADH (ADH antagonists)
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24
Q

Carbonic Anhydrase Inhibitors

A

Acetazolamide
MOA: Inhibit Carbonic Anhydrase, HCO3- stays in lumen, less H20 reabsorbed in tubule
SOA: Proximal convoluted Tubule
Note: SULFA DRUG (watch for allergies)

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25
Q

Osmotic Diuretics (Aquaretic)

A

Mannitol
MOA: Draws free H20 thus increase Urine Flow
SOA: PCT & Descending loop of henle
CI: HF and Pulmonary edema (due to Mannitol-Induced Extracellular volume expansion)
Glycerol
MOA: Draws free H20. can be metabolized!
Usually used for cerebral edema

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26
Q

Loop Diuretics

A

SOA: TAL
1. Furosemide (20-40mg)
MOA: Inhibit Na+/K+/2Cl- cotransporter. TAL impermeable to water. Loss of volume with a positive potential. SULFA DRUG.
2. Ethacrynic acid
MOA: Inhibit Na+/K+/2Cl- cotransporter but not Sulfa drug. give to Sulfa-sensitive pts

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27
Q

Loop Diuretics Side effects & CI

A

OHH DAANG
Ototoxicity, Hypokalemia, Hyponatremia, Dehydration, Allergy, contraction Alkalosis, Nephritis (interstitial), Gout (hyperuricemia - uric acid crystals).
Ethacrynic acid is more ototoxic
CI: NSAIDs (due to COX-2), Lithium (enhanced effects), Aminoglycoside (otoxicity), Digoxin (electrolyte imbalance)

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28
Q

Thiazide diuretics

A

SOA: DCT
1. Hydrochlorothiazide (in hypertension 6,25-25mg
in congestive heart failure 25-100mg)
2. Indapamide (thiazide-like diuretic) - More for HTN and can combine with ACE inhibitor
MOA: Inhibit Na+/Cl- cotransporter, low diluting nephron capacity, decrease Ca excretion
SULFA DRUGS

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29
Q

Thiazide diuretics SE & CI

A

SE: HyperGLUC
Contraction alkalosis, hyponatremia, hyperGlycemia, hyperLipidemia, hyperUricemia, hyperCalcemia, sulfa allergy
CI: Digoxin (electrolyte imbalances), DM pts (decrease Insulin release by opening K+ channels)

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30
Q

K+ - sparing diuretics

A
  1. Aldosterone receptor Inhibitors (MRA): Spironolactone, Eplerone
  2. ENaC Inhibitors (Amiloride)
    SOA: Collecting duct (principal& intercalated cells)
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31
Q

Aldosterone R. Inhibitors Uses

A
  1. Hyperaldosteronism (Conn’s Sy)
  2. Hypokalemia from other diuretics
  3. Congestive HF (inhibits cardiac remodelling)
  4. Antiandrogenic use (inhibit 17alpha hydroxylase -PCOS, Female hirutism)
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32
Q

ENac Inhibitor Uses

A
  1. Hypokalemia
  2. NDI
  3. Liddle’s sy. (too many ENaCs)
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33
Q

Which channels do Aldosterone Receptor Inhibitors affect?

A
  1. Na+/K+ ATPase
  2. ENaC
  3. K+ channels on apical membrane
  4. H+ ATPase (intercalated cell)
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34
Q

ADH antagonists (MOA, SOA, SE)

A

Tolvaptan
MOA: Selective V2R antagonist. ADH cannot bind, no AQP2, promote free water excretion
SOA: Collecting Duct
Use: SIADH & correct hyponatremia
SE: Hypernatremia, Central Pontine Myelinolysis

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35
Q

Types of Antiarrhythmic drugs

A
  1. Class I - Na+ channel blockers (Rhythm control)
  2. Class II - beta blockers (Rate control)
  3. Class III - K+ channel Blockers (Rhythm control)
  4. Class IV - Ca channel blockers (Rate control)
  5. Class V - Others (adenosine, Mg2+, K+, Digoxin - Rate control)
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36
Q

Class I antiarrhythmics

A

Class IA - Quinidine
Class IB - Lidocaine (preferance for ischemic tissue)
Class IC - Propafenone (CI in pts with ischemic tissue. Proarrhythmogenic effects)
NOTE: Widened QRS complex on ECG

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37
Q

Class II antiarrhythmics

A

beta blockers
1. Cardioselective: Esmolol (IV. acute arrhythmia and intraoperative)
2. Non-selective: Propanolol (Oral. Post-MI to avoid Ventricular Fibrillation)
Note: Can cause Heart Block, presents as prolonged PR interval

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38
Q

Class III Antiarrhythmics

A

MOA: Inhibit K+ channels in phase 2 and phase 3 (thus slowed down. Prolonged refractory period)
1. Amiodarone (Shares properties from Classes I, II, III & IV. Lots of SE)
2. Sotalol (Both a Class III and a beta blocker -> Decrease HR & AV conduction)
NOTE: Can widen QT interval

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39
Q

Amiodarone Side Effects

A
  1. Lung fibrosis - Restrictive Lung disease
  2. Hepatotoxicity - Hypersensitivity Hepatitis
  3. Hypo/Hyperthyroidism
  4. Blue/Gray deposits on cornea/skin
  5. Photodermatitis
  6. AV Block
  7. Torsades
  8. Inhibit CYP450 so interfere with other CYP450 drugs
  9. Induce Heart Failure
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40
Q

Class IV Antiarrhythmics

A

Verapamil

MOA: Inhibit Ca channels, slow down phase 0 and phase 4 - Rate control + Decrease cardiac contractility and BP

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41
Q

Class V Antiarrhythmics

A
  1. Adenosine: A1R activation -> hyperpolarization-> inhibit Ca channels. 1st line agent for acute supraventricular tachys
  2. Digoxin: Direct stimulation of vagus nerve
  3. K+
  4. Mg2+ : can treat torsades and digoxin toxicity
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42
Q

Order of treatment for Rate control of AF

A

1st line: Class II or Class IV

2nd line: Digoxin

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43
Q

Hypertensive Treatment

A

Primary HTN: Thiazides, ACE inh/ARBs, DHP Ca Ch. Blockers
HTN with HF: Diuretics, ACE/ARBs, beta blockers (ONLY COMPENSATED HF), MRAs
HTN with DM: ACE/ARBs, Ca ch. blockers, beta blockers
HTN with Asthma: ARBs. Ca ch. blockers, thiazides, selective beta blockers
HTN in pregnancy: Methydopa, nifedipine

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44
Q

Types of Antihypertensives

A
  1. Diuretics (Thiazides/ Loop)
  2. Sympatholytics
  3. Vasodilators
  4. RAAS system drugs
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45
Q

HTN emergency management

A

All drugs are given IV.

  • Beta blockers (esmolol)
  • Ca ch. blockers (Nicardipine)
  • Nitroprusside
  • Hydralazine
  • ACE Inhibitors (captopril)
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46
Q

Ca channel Inhibitors

A

MOA: Inhibit L-Type Ca channels in smooth muscle cells (vessels) and on heart

  1. Dihydropyridine (DHP) - more vascular effect
  2. Non-dihydropyridines - more cardiac effect
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47
Q

DHPs (names, uses, SE)

A
  • Nifedipine: short acting. Do not give in MI or unstable angina pts due to reflex tachycardia. Can give to pregnant women
  • Nicardipine: give as IV in HTN emergency
  • Felodipine
  • Nimodipine
  • Amlodipine (long-acting) - 1×5-10mg
    Uses:HTN, Raynud syndrome, Prinzmental&Stable angina, Subarachnoid hemorrhage (prevent vasospasm), HTN emergency
    SE: Ankle (Peripheral) edema, light-headedness, reflex tachy
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48
Q

Non-DHPs (names, uses, SE)

A

Verapamil
Rate control @ AV&SA nodes (lower HR - Brady), decrease cardiac contractility, decrease myocardial oxygen demand
SE: Constipation, Gingival Hypertrophy, Worsen HF, AV Block if given with beta-blockers, CI in pts with pre-existing heart block

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49
Q

Vasodilating drugs for HTN treatment (Not CCB)

A
  1. Nitric Oxide releasing agents (Hydralazine)
  2. Endothelin antagonists (Bosentan)
  3. PDE-5 Inhibitors (Sildenafil)
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50
Q

RAAS pathway drugs as antihypertensives

A
  1. ACE Inhibitors (Captopril, Enalapril, Perindopril, Ramipril)
  2. ARBs (Losartan, Valsartan in combo w/ Sacubitril - ARNi, Irbesartan)
  3. MRAs (Spironolactone, Eplerenone)
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51
Q

Angina pectoris (Ischemic Heart Disease) drug treatment

A
  1. Nitrates (nitroglycerin - 0.5mg sublingual & isosorbide dinitrate)
  2. Ca channel blockers (Nifedipine, Verapamil)
  3. Beta blockers (Propanolol)
  4. Trimetazidine (MOA: partial fatty acid oxidation inhibition - pathway goes into glucose oxidation, less O2 consumption, optimize cellular energy processes)
  5. Ivabradine (MOA: Inhibit If Na channels in SA node-> Hyperpolarization-> Lower HR -> Decreased O2 demands)
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52
Q

Nitrates SEs and CIs

A

SE: Headaches, flushing, reflex tachy (prevent with beta blockers), orthostatic HypoTN, methemoglobinemia, tolerance
CI: Systolic BP <90mmHg, Right ventricular MI, Pt taking PDE-5 inhibitors within 24hours, Hypetrophic obstructive cardiomyopathy

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53
Q

Dyslipidaemia Drugs

A
  1. Statins
  2. Bile acid sequestrants-Resins
  3. Sterol absorption inhibitors
  4. Fibrates
    (not in topic list but 5. Niacin and 6. Others eg Folic acid)
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54
Q

Statins

A

Simvastatin, Atorvastatin, Rosuvastatin (CYP450 DRUGS)
MOA: Inhibit HMG-CoA Reductase, Increase LDL-R Expression (increase cholesterol uptake by liver)
Effect: Highest decrease in LDL, small increase in HDL, small decrease in TGA
Use: CAD pts to increase survival, decrease risk of atherosclerosis & PAD, high risk diabetics
SE: hepatotoxicity, myopathy
CI: Pregnancy, liver disease pts

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55
Q

Bile acid sequestrants - resins

A

Colesevalam
MOA: Bind on bile acids and inhibit absorption in the intestine. Liver uses up its cholesterol to make new bile acids. Lower LDL. Increase LDL-R expression
SE: Constipation, Bloating, Decreased absorption of fat-soluble vitamins (DEAK), Increase VLDL & TGA, Cholesterol gallstones

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56
Q

Sterol Absorption Inhibitors

A

Ezetimibe
MOA: Bind NPC1L1 transporter. Less cholesterol absorption. Liver forced to make own cholesterol. Increase LDL-R Expression. Decrease circulating LDL
SE: Steatorrhea, Increased LFTs

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57
Q

Fibrates

A

Fenofibrate
MOA: PPAR-α agonist. Upregulate LPL -> Hydrolyze VLDL&TGA -> Free fatty acids used up by heart and skeletal muscle for energy
Decrease VLDL & TGA
SE: Cholesterol gallstones, Increased myopathy risk if used with statins

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58
Q

Histamine actions

A
  1. Type I allergic rxn (IgE mediated)
  2. Increase Vascular permeability
  3. Bronchial muscle constriction
  4. Increase Nasal&Bronchial mucous production
  5. Neurotransmitter (mediate sleep/arousal)
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59
Q

Antihistamine drugs

A

H1R antagonists (1st & 2nd gen)

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60
Q

1st generation H1R antagonists

A
  1. Diphenhydramine
  2. Promethazine (more sedative/autonomic effects)
  3. Dimetindene (less sedative. more allergy txt)
    MOA: inhibit central & peripheral H1Rs,Inhibitory effects of alpha1R (dizziness& HypoTN), Musc-R inhibitory effect, serotonin-R inhibitory effects (increase apetite & weight gain). CYP450 DRUGS.
    Use: IgE allergies, sedative, antiemetic, sleep-aid, anti-motion sickness, control of nausea&vomiting in pregnancy, manage acute extrapyramidal sxs
    SE: Sedation, antimuscarinic effects, Interaction with BZDs&alchohol)
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61
Q

2nd generation H1R antagonists

A
  1. Cetirizine
  2. Loratadine
  3. Fexofenadine
    MOA: Inhibit peripheral H1Rs. Do not cross BBB so no autonomic/anti motion sickness effects. CYP450 DRUGS.
    Use: IgE med. allergies
    SE: Sedation, arrhythmias in overdose, interact with other sedatives
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62
Q

Cholinergic Transmission NT and Receptors

A

NT: Acetylcholine
Receptors: Nicotinic and Muscarinic (Sympathetic and Parasympathetic postganglionic fibers)

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63
Q

Cholinomimetics

A
  1. Carbachol (MR &NR) - open angle glaucoma

2. Pilocarpine (MR) - closed angle glaucoma, xerostomia

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64
Q

Anticholinesterases (Indirect agonists)

A

MOA: Inhibit Acetylcholinesterase, enhance nAchR activity
Tertiary: Rivastigmine (Alzheimers) & Physostigmine (anticholinergic atropine toxicity - central&peripheral)
Quarternary: Neostigmine (urinary retention, ileus, Myasthenia Gravis, Curare reversal), Edrophonium (MG Tensillon test)

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65
Q

Antimuscarinics

A

MOA: Reversible block. Block Parasympathetic activation

  1. Atropine (M3R-Eye & M2R-Heart): mydriasis, increase HR & AV conduction. Dose 0,3-1,0mg
  2. Ipratropium, Tiotropium (M3R-Lung): Bronchodilation
  3. Oxybutynin, Solifenacin (M3R-Genitourinary): Reduce urinary incontinence
  4. Scopolamine(transdermal), Butyl-scopolamine(oral): M1R-CNS, Motion Sickness
  5. Cyclopentolate (M3R-Eye): Cycloplegia
  6. Procyclidine (M1R-CNS): Parkinson’s
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66
Q

Catelcholamines

A
  1. Epinephrine (β2&αRs dose dependent) - Anaphylactic shock - sc. or im. 0,15-0,5mg, iv. 0,05-0,1mg
    resuscitation 1mg
  2. Norepinephrine (α1>α2, β1) - Septic Shock
  3. Isoprenaline (β1= β2) - Cardiac arrest, complete heart block
  4. Dobutamine (β1> β2) - Cardiogenic shock
  5. Dopamine (indirect. D1R, β1 @low dose. D2R @high dose) - increase CNS activity, Increase renal blood flow
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67
Q

Indirect sympathomimetics

A

Ephedrine (Decongestant, HypoTN, stimulant)
MOA: Displace stored catelcholamines from nerve endings
Phenylephrine (HypoTN, Rhinitis, ischemic priapism)

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68
Q

Selective α2 agonists

A

MOA: Bind to α2Rs to decrease sympathetic tone
1. Clonidine - HTN Emergency, Tourette’s & ADHD
SE: bradycardia, HypoTN, Decrease CNS action (also binds to I1R)
2. α-Methyldopa - Gestational HTN
SE: Drug-induced lupus
3. Rilmenidine - HTN
SE: milder than Clonidine
Note: Acts on Imidazole R (I1)
4. Oxymetazoline - Decongestant
SE: Only when given systemically, HypoTN

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69
Q

α-Receptor antagonists

A
  1. Non-selective : Phentolamine - Pheochromocytoma pre-op, Antidote for HTN due to α-agonist OD
    SE: Orthostatic hypoTN
  2. α1-selective: Prazosin, Doxazosin, Tamsulosin - HTN, BPH, Prazosin for PTSD
    SE: Orthostatic hypoTN
  3. α2, α1,β: Urapidil + 5-HT weak agonist - HTN, BPH
  4. Both α &β: Carvedilol - HTN Emergency, decrease variceal bleeding, decrease mortality in HF
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70
Q

β-Receptor antagonists

A
  1. Non-selective
    - Propanolol (Angina, Class II Antiarrhythmic, HTN, thyroid storm, Migraine Prophylaxis, Tremor)
    - Timolol (glaucoma)
    - Pindolol (HTN in asthma/COPD pts, CI IN HF!!)
    - Sotalol (Also a K+ ch antagonist - Class III Antiarrhythmic. SE: Torsades)
  2. β1 selective - cardioselective
    - Metoprolol ( 2×25-100mg) , Bisoprolol, Nebivolol (HTN, CHF, Angina, Anti-arrhythmics Class II, ACS)
    - Esmolol (IV, HTN Emergency, thyroid-storm arrhythmias)
  3. β&α combined
    - Carvedilol (CHF, Reduce mortality)
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71
Q

Centrally acting Skeletal muscle relaxants (Spasmolytics)

A
  1. Baclofen: GABA-b. Cerebral palsy, MS. SE: Sedation, rebound plasticity
  2. Diazepam: GABA-a. Chronic&Acute spasm. SE: CNS depressant, tolerance & dependence
  3. Tizanidine: α2 agonist. MS, Stroke. SE: sedation, hypoTN, rebound HTN
  4. Tolperisone: Na+ & Ca+ ch blocker. Acute spasm. SE: Strong antimuscarinic effects
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72
Q

Direct acting muscle relaxants

A
  1. Dentrolene
    MOA: RyR1 antagonist -> block Ca+ release in SR -> less actin-myosin interaction
    Use: Malignant Hyperthermia. SE: Hepatotoxic
  2. Botulinum toxin
    MOA: inhibit SNARE to prevent synaptic exocytosis -> Flaccid paralysis
    Use: spasm, migraine, cosmetics, hyperhidrosis
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73
Q

Skeletal Muscle Relaxants acting on the NMJ

A
  1. Non depolarizing - competitive antagonists at sk muscle nAchRs (Nm) aka. Curare type
  2. Depolarizing - agonist at Nm, can stimulate ganglionic nAchR and cardiac M3R
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74
Q

Non-depolarizing NMJ anesthetics

A
  1. Mivacurium - short acting. Pseudocholinesterase
  2. Rocuronium - IM acting. hepatic metabolism
  3. Cisatracurium - IM acting. spontaneous metabolism.
  4. Atracurium - IM acting. spontaneous.
  5. Piperacurium - long acting. renal metabolism

SE: Histamine release (HypoTN), Prolonged apnea, Tachy

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75
Q

Depolarizing NMJ Anesthetics

A

Succinylcholine (Suxamethonium)
Parenteral with 5-10 min duration. metabolized by cholinesterase enzymes
Use: Surgery with brief duration, Status epilepticus
SE: Arrhythmias, malignant hyperthermia

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76
Q

Types of local anesthetics

A
  • Amides
  • Esters

Order of nerve blockade: A delta, C, A beta (prefer small, myelinated nerve fibers)

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77
Q

Amide local anesthetics

A
  1. Lidocaine (short acting) - CYP450 drug
  2. Articaine (short acting, most rapid onset of all LA)
  3. Bupivacaine (longest acting, most potent, CNS toxicity, CYP450 drug)
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78
Q

Ester Local anesthetics

A
  • Cocaine

Surface acting, metabolized by pseudocholinesterase, only LA that’s vasoconstricting

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79
Q

Glucocorticoids (-sone suffix)

parenteral & oral

A
  1. Hydrocortisone - short acting, replacement therapy in adrenal insufficiency
  2. Prednisolone - IM acting
  3. Methylprednisolone - IM acting (4-250 mg)
  4. Triamcinolone - IM acting. Usually topical. High toxicity compared to others
  5. Dexamethasone - Long acting
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80
Q

Topical Glucocorticoids

A
  1. Fluocinolone
  2. Budesonide
  3. Mometasone
  4. Fluticasone
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81
Q

Mineralocorticoids

A
  1. Aldosterone (endogenous)

2. Fludrocortisone

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82
Q

Corticosteroid Antagonists

A
  1. MRA antagonists (spironolocatone& eplerone)

2. Metyrapone (11 beta hydroxylase inhibition)

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83
Q

Androgens

A
  1. Testosterone-undecanoate (testosterone analogue)
  2. Nandolon (anabolic steroid)
  3. Bicalutamide (Testosterone Receptor Inhibitor)
  4. Finasteride (5alpha reductase inhibitor)
  5. Goserelin (GnRH analogue)
  6. Degarelix (GnRH antagonist)
  7. Sildenafil (PDE-5 Inhibitor, Help with Erectile dysfunction)
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84
Q

Estrogens and Antiestrogens

A
  1. Ethinyl-estradiol (CYP450 metabolism)
  2. Estradiol
  3. Tamoxifen (SERM, Hormone-responsive breast cancer)
  4. Raloxifen (SERM, Osteoporosis in post-menopausal women)
  5. Clomifene (SERM, ovulation induction)
  6. Anastrozole (Synthesis Inhibitor-Aromatase, Hormone Responsive breast cancer adjuvant)
  7. Goserelin (GnRH analogue, Ovarian suppression, central precocious puberty)
  8. Degarelix (GnRh antagonist, Controlled ovarian stimulation)
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85
Q

How SERM (Selective Estrogen Receptor Modulators) work

A

Estrogen antagonist @ breast, CNS, uterus

Estrogen agonist @liver, bone

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86
Q

Progestins

A

3 types:
1. Pregans - Medroxyprogesterone-acetate, Drospirone, Cyproterone-acetate
2. Estrans - Norethisterone
3. Gonans - Desogestrel, Levonogestrel
MOA: Bing progesterone Rs, decrease growth & increase vascularization of uterus

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87
Q

Antiprogestins

A
  1. Mifepristone (Glucocorticoid&Progesteron R antagonist)
    Medical abortion in combo with PGE analogue
  2. Ulipristal acetate (SPRM)
    Day after pill, myoma growth suppression
88
Q

Oral Hormonal Contraceptives

A
  1. Combined: Ethinyl Estradiol + Progestin (Levonorgestrel, Desogestrel, Dosperidone)
  2. Minipill (progestin only)
89
Q

Other contraceptives

A
  1. Depot Injection - Medrocyprogesterone-acetate

2. IUD -levonorgestrel

90
Q

Thyroid and antithyroid drugs

A
  1. Levothyroxine (T4) - give in hypothyroidism (25-150 µg)
  2. Propythiouracil (PTU) - inhibit TPO and 5’ deiodinase (hyperthyroidism)
  3. Methimazole (Thiamazole) - inhibit TPO
91
Q

How to treat thyroid storm (untreated hyperthyroidism)

A
  1. Beta blockers (propanolol) - treat SNS effects
  2. PTU/Methimazole - decrease T3&T4 levels
  3. Glucocorticoids (hydrocortisone) - treat opthalmopathy
  4. KI

All given IV. PTU & Methimazole given bolus IV

92
Q

Anterior Pituitary Hormone Drugs

A

GH antagonist:
Octreotide - Inhibit release of GH, Insulin, Glucacon, Gastrin
Prolactin antagonist:
Bromocriptine - D2R agonist, inhibit pituitary secretion of prolactin

93
Q

Posterior Pituitary Hormone Drugs

A
  1. Oxytocin - Oxytocin receptor agonist. Increase uterine contractions & induce labor/ control uterine hemorrhage
  2. Desmopressin - ADH agonist (V2R). Treat Nephrogenic DI, Haemophilia A & VWF Disease
94
Q

Anticoagulant drugs types

A 
1. Heparin
MOA: Inhibit formation of fibrin clots. Bind ATIII, inhibit factors IX, XI, XII &amp; Plasmin
2. Direct acting thrombin inhibitors
3. Direct acting Factor Xa inhibitors
4. Coumarin - Warfarin
95
Q

Heparin drugs

A
  1. Unfractionated heparin (highest chance of HIT. use for DVT, PE, acute MI)
  2. Dalteparin - Low molecular weight heparin (watch out for renal insufficiency)
  3. Fondaparinux (high specificity to factor Xa)

REVERSE: Protamine Sulfate

96
Q

Direct acting thrombin inhibitors

A
  1. Bivalirudin (anticoagulation in pts with HIT. Give with aspirin during PCI)
  2. Dabigatran-etexilate (chronic therapy for AF to prevent clot formation)
97
Q

Direct acting factor Xa inhibitors

A

Rivaroxiban (prevent venous thromboembolism post-op, prevent stroke in AF)

98
Q

Warfarin uses

A

CHRONIC anticoagulation (AF, Thrombi, VTE, Post-Mi, heart valve damage)

CYP450 DRUG!
REVERSE: Vitamin K, FFP, PCC

99
Q

Antiplatelet drugs

A
  1. COX inhibitors (Acetylsalicylic acid)
  2. Glycoprotein IIb/IIIa Inhibitors (Abciximab)
  3. ADP-R antagonists (clopidogrel, prasugrel, ticagrelor)
100
Q

Fibrinolytics (-teplase)

A
  1. Alteplase
  2. Reteplase

MOA: tPAs convertin plasminogen into plasmin.
Pernteral.
USE: Acute MI if cannot PCI within 2 hrs. Ischemic stroke. PE (haemo instability), DVT
CI: Cerebral hemorrhage/recent intracranial surgery
SE: Cerebral hemorrhage

101
Q

Bleeding Disorder Drugs

A
  • Vitamin K
    Oral/Parenteral
    Reverse excessive warfarin anticlotting activity/ Vit K deficiency
  • Antiplasmin drugs
    MOA: Inhibit plasminogen activation -> No fibrinolysis
    1. Aminocaproic acid - Reverse fibrinolysis, use in acute bleeding episodes
    CI: DIC, Bleeding of upper urinary tract
    SE: Thrombosis, HypoTN, diarrhea
    2. Epinephrine
    3. Fibrin Foam
102
Q

Anemia drugs

A
  1. Iron - Iron hydroxylide Polymaltose Complex
  2. Vitamin B12 (cobalamin)
  3. Folic acid (Vitamin B9)
  4. Epoetin alpha
  5. Filgrastim
103
Q

Parenteral drugs for IDDM

A
  1. Insulin Lispro (Rapid acting)
  2. Regular Insulin (short acting)
  3. NPH-Insulin (IM acting) - combo w/ short acting
  4. Insulin Glargine (long acting)
  5. Liraglutide (GLP-1 analogue)
104
Q

Oral antidiabetics

A
  1. Insulin secretagogues:
    a) Sulfonylureas (2nd gen - Glimepiride, Glipizide)
    b) Meglitines: Repaglinide
  2. Biguanides: Metformin (2-3×500-850mg)
  3. DPP-4 Inhibitor: Vidagliptin
  4. SLGT-2 Inhibitors: Dapagliflozin
  5. alpha-glucosidase Inhibitora: Acarbose
105
Q

Agents affecting bone mineral homeostasis

A
  1. Teriparatide - PTH analogue
  2. Cholecalciferol - Vitamin D3
  3. Raloxifene - SERM
  4. Alendronate & Zoledronate - Bisphosphonates
  5. Denosumab - IgG Ab
  6. Calcitonin
106
Q

1st line treatment in osteoporosis

A

Bisphosphonates

107
Q

Osteoporosis pharmacotherapy - Inhibit Bone resorption

A
  1. Hormone Replacement therapy
  2. SERM
  3. Bisphosphonates
  4. RANK-L Inhibitors
  5. Calcitonin analogues
108
Q

Osteoporosis pharmacotherapy - Increase bone formation

A
  1. Teraparatide
  2. Ca2+ supplements
  3. vitamin D supplements
  4. Thiazides diuretics
109
Q

Autoimmne Disease Drugs

A
  1. Cyclophosphamide (Alkylating agent)
  2. Methotrexate (Folate antimetabolite. Inhibit DHF reductase. S-phase)
  3. Leflunomide (Inhibit de novo pyrimidine synthesis)
  4. Azathioprin (-> 6-MP. Inhibit conversion of PRPP->IMP. No RNA/DNA synthesis. S phase)
  5. Mycophenolate - mofetil (IMP dehydrogenase. Less GMP, less WBC proliferation)
110
Q

Cytokine gene expression & 5-ASA derivatives

A
  1. Cyclosporin A (bind cyclophilin, Calcineurin Inhibitor)
  2. Tacrolimus- FK506 (Bind FK-binding protein. Calcineurin inhibitor)
  3. Sirolimus (mTOR inhibitor)
  4. Tofacitinib (Inhibit JAK1&3)
  5. Sulfasalazine ( PPAR-γ agonist - Less TLRs&NFkB, Less cytokine, Inhibit COX&LOX. 5-ASA derivative)
111
Q

Antibodies & Fusion Proteins

A
  1. ATG (Bind T-cells. Serum complement destruction)
  2. Rituximab (Anti-CD20. Monoclonal Chimeric)
  3. Infliximab (Anti-TNFa. Monoclonal Chimeric)
  4. Adalizumab (Anti-TNFa. Human)
  5. Tocilizumab (Anti-IL6 receptor)
  6. Ustekinumab (Anti-IL12&23)
  7. Natalizumab (Anti-integrin a4b1. Inhibit WBC entry via BBB)
  8. Dupilumab (Anti-IL4 Ra)
  9. Abatacept (fusion protein. CTLA-4 fusion protein, Bind CD80/86 on APC)
112
Q

Chemo - Antimetabolites

A
  1. 5-Fluorouracil (Inhibit Thimydilate synthase) - combine with leucovorin for max effect
  2. Capecitavine (Bioactivated to 5-FU)
  3. Cytarabine (Inhibit DNA polymerase)
  4. 6-Mercaptopurine (Inhibit Purine Metabolism)
  5. Methotrexate ( Inhibit DHF Reductase)
  6. Pemetrexed (Folate antimetabolite)
113
Q

Chemo - Alkylating agents

A

Interrupt DNA/RNA cross linking
1. Cyclophosphamide (CCNS, Nitrogen mustard)
2. Dacarbazine
3. Temozolamide
4. Bleomycin (Antitumor antibiotic. Free radicals. Pulmonary probs)
5. Dactinomycin (Antitumor antibiotic)
6. Cisplatin & Oxiplatin (inter & intra- strand interruption)
CISPLATIN DOES NOT CAUSE MYELOSUPPRESSION

114
Q

Chemo - Topoisomerase Inhibitors

A
  1. Etoposide (Inhibit Topoisomerase II) - G2 phase
  2. Irinotecan (Inhibit Topoisomerase I) - S phase
  3. Doxorubicin (antitumor antibiotic. Inhibit Topoisomerase II)
115
Q

Chemo - Mitotic Spindle Inhibition

A
  1. Vincristine (vinca alkaloid, Inhibit MT polymerization)
  2. Docetaxel (Inhibit MT degradation so no mitotic spindle formation)
    Both M-phase
116
Q

Chemo - Hormonal agents

A
  1. Prednisolone (corticosteroid)
  2. Tamoxifen (SERM) - only one given to pre-menopausal women
  3. Anastrozole (Aromatase inhibitor)
  4. Goserelin (GnRH agonist - continuous)
  5. Degareliz (GnRH antagonist)
  6. Bicalutamide |(oral non-steroidal antiandrogen)
  7. Octreotide (Somatostatin analogue)
117
Q

Chemo - Small molecules

A
  • Tyr-Kinase Inhibitors on Intracellular domain*
    1. Imatinib (BCR-ABL t(9;22) )
    2. Gefitinib & Erlotinib (EGFR antagonists)
    3. Lapatinib (Her2/neu & EGFR antagonist)
    4. Sunitinib (VEGFR & PDGFR)
    5. Ibrutinib (Bruton’s kinase on B-cells)
    6. Crizotinib (ALK Kinase & ROS1 oncogene)
    7. Bortezamin (Inhibit proteosomal activation of NFkB)
    8. Dabrafenib & Trametinib combo (BRAF & MEK - melanoma)
    9. Everolimus (Sirolimus derivative, mTOR inhibitor)
    10. Tretinoin (Vit A derivative - promyelocyte differentiation)
118
Q

Chemo - large molecules

A
  • Monoclonal Abs. All human except Rituximab*
    1. Transtuzumab (Herceptin - AntiHER2/neu)
    2. Panitumumab (Anti-EGFR)
    3. Rituximab (Anti CD20 - B-cells)
    4. Bevacizumab (Anti-VEGF)
    5. IFN alpha (antineoplastic, antiviral, immunosuppressant)
    6. Aldesleukin (IL-1 recombinant protein)
    7. Pembrolizumab (Immunomodulator. PD-1 binding)
119
Q

Opioid analgesics - Natural

A
  1. Morphine - MorphineSO4 oral: 2×30-100mg, Morphine HCL iv: 10-20mg
  2. Codeine (anti-tussive)
120
Q

Opioid analgesics - semisynthetic

A
  1. Hydromorphone (analgesia)
  2. Oxycodone (abuse)
  3. Dihydrocodeine (antitussive)
  4. Buprenorphine (withdrawal symptom management)
  5. Nalbuphine (spinal anesthesia)
121
Q

Opioid μ analgesics - synthetic

A
  1. Fentanyl (transdermal/sublingual - anesthesia)
  2. Tramadol (chronic pain)
  3. Meperidine/Pethidine (analgesia in ER)
  4. Loperamide & Diphenoxylate (Anti-diarrheals - Loperamide has no CNS effects)
  5. Methadone (opioid withdrawal management)
122
Q

Opioid antagonists

A
  1. Naloxone (IV. reverse opioid OD)

2. Methyl-naltrexone (Reduce nicotine and alcohol cravings + maintenance)

123
Q

Gout drugs

A
  1. Colchicine (Inhibit MT assembly)
  2. Allopurinol (Xanthine Oxidase inhibitor)
  3. Rasburicase (Urate oxidase recombinant)

In acute gout attacks, give intraarticular steroids (prednisone)

124
Q

Non-opioid analgesics (NSAIDs)

A
  1. Aspirin (acetylsalicilic acid - irreversible inhibition) dose dependent drug; For inhibiting the platelet aggregation 50-200mg
    Analgesic and antipyretic dose 500mg)
  2. Ibuprofen (pediatrics) 1-4×200-600mg
  3. Indomethacin (Acute gout attack. Closure Ductus Arteriosus)
  4. Naloxen (Acute gout. Dysmenorrhea)
  5. Diclofenac (MSK pain) 2-3x50mg
  6. Metamizole 500-1000mg
  7. Ketoprofen (-dex) (lower LTs)
  8. Phenylbutazine (Can cause aplastic anemia!)
  9. Meloxicam (more inhibition on COX-2)
  10. Celecoxib (Cox-2 selective)
  11. Acetaminophen (no peripheral COX inhibition)
    1-4×500-1000mg
125
Q

Acetaminophen toxicity antidote

A

N-acetylcysteine

126
Q

Salicylate toxicities (OD)

A

Tinnitus, abdominal pain, fever, Double acid-base disorder (mixed)
Treat with Activated charcoal and IV NaHCO3

127
Q

Antacids

A
  1. Mg (OH)2
  2. Al(OH)3

Decrease Warfarin & Tetracyclines absorption. Increase Quinidine absorption

128
Q

Proton Pump Inhibitors

A
  1. Omeprazole (prodrug. Can inhibit clopidogrel activation)

2. Pantoprazole (oral and iv); ORAL: 2×20-40mg

129
Q

H2Receptor inhibitors

A

Famotidine (decrease NOCTURNAL acid secretion) 2x20mg or 1x40mg

130
Q

Laxatives

A
  1. Senna/ sennoside
  2. Bicasodyl
  3. Plant fiber
  4. MgSO4
  5. Lactulose
  6. Paraffin oil (pt must be upright when ingesting; avoid Lipoid pneumonia)
131
Q

Antidiarrheals

A
  • μ-opioid agonists in GI*
  1. Loperamide (no BBB cross)
  2. Diphenoxylate (Must combine with Atropine to avoid CNS effects)
  3. Activated charcoal
132
Q

Antiemetics

A
  1. Diphenhydrinate (H1R blocker - combo of diphenhydramine&theophylline)
  2. Onsanserton (oral/IV) & Palonoserton (IV) - Inhibit 5HT3Rs in GI
  3. Metoclopramide (Inhibit D2Rs. Prokinetic at low dose, Antiemetic at high dose)
  4. Dropiredol (Inhibit D2Rs, antipsychotic)
  5. Aprepitant (Inhibit NK1R at area postrema) - CYP450 inhibitor
  6. Cannabinoid (agonist of CBRs, inhibit presyntaptic DA - AIDS wasting syndrome)
133
Q

Abdominal & Urogenital painkillers /spasmolytics

smooth muscle drugs

A
  1. Butylscopolamine (Anticholinergic non-selective w/o CNS penetration)
  2. Solifenacin & Oxybutynin (M3R inhibitors. transdermal patch)
  3. Papaverine (CCB, inhibit PDE. Oral/IV)
134
Q

Tocolytics (Smooth muscle drugs)

A
  1. Atosiban (Oxytocin R antagonist - IV)
  2. Terbutaline ( SABA - IV/pos)
  3. MgSO4 (IV - also used to prevent seizures in preeclampsia)
  4. Ethanol (IV)
135
Q

Uterine contractants (Smooth muscle drugs)

A
  1. Oxytocin (Oxytocin R agonist - IV/intranasal)
  2. Ergotamine (Vasoconstrictor- alphaR agonist &partial @ 5TH2, Ergot alkaloid - IV)
    NOTE: DO NOT GIVE BEFORE PLACENTA DELIVERY
  3. Misoprostol (PGE1 analogue - Oral)
    Note: combined with Mifepristone for abortion
136
Q

BPH Smooth muscle drugs

A

Tamsulosin (uroselective alpha1 blocker - oral)

137
Q

Liver & Biliary tract drugs

A
  1. N-acetylcysteine - acetaminophen toxicity/mucolytic
  2. Ursodiol (Decrease cholesterol absorption - CI: Acute hepatitis & biliary obstruction!!)
  3. Silimarin (antidote to amanita phalloides - support liver function)
138
Q

Alzheimer’s drugs

A
  1. Rivastigmine (Cholinesterase inhibitor, tertiary, cross BBB)
  2. Memantine (NMDA-R Blocker)

Nootropic - Piracetam (cognition enhancer)

139
Q

Parkinson’s drugs (precursors and endogenous release)

A
  1. Levodopa (DA precursor) - do not give in psychosis
  2. Carbidopa (DA DC inhibitor) combined with Levidopa
  3. Amantadine (Potentiate endogenous DA & NMDARs inhibitor - less glutamate)
140
Q

Parkinson’s - DA R agonists

A
  1. Ropinirole (D2R agonist - non ergot)

2. Pramipexole (D3R agonist - non ergot)

141
Q

Parkinson’s MAO-I, M1Rs & COMT inhibitor

A
  1. Selegiline (MAO-B inhibitor)
  2. Entecapone (COMT inhibitor - peripheral)
  3. Procyclidine & Benztropine (inhibit M1Rs - less tremor/dyskinesia)
142
Q

Anticonvulsants - Grand mal txt

A
  1. Valproic acid (Inhibit Na chs, T-type Ca2+ chs, GABA transaminase, Increase K+ permeability in neurons)
  2. Phenytoin (Inhibit axonal Na+ chs - does not stop initiation of seizure. Non-linear kinetics)
  3. Carbamazepine (Inhibit Na+ chs, no inhibition of initiation
  4. Lamotrigine (AMPA-R glutamate antagonist & Inhibit Na+ chs - requires hepatic glucorunidation)
143
Q

Anticonvulsants - Petit mal

A
  1. Ethosuximide (Inhibit T-type Ca2+ chs in thalamus)
  2. Clonazepam (BZD - long acting)
  3. Valproic acid
144
Q

Anticonvulsants - Myoclonic seizures

A
  1. Clonazepam
  2. Lamotrigine
  3. Valproic acid
145
Q

Status epilepticus treatment

A
  1. Bolus IV lorazepam/ midazolam/ diazepam

2. IV continuous for 5-20’ : Phenytoin/ Levetiracetam

146
Q

Anticonvulsants - miscalleneous

A
  1. Vigabitrin (Inhibit GABA transaminase - partial & grand mal)
  2. Levetiracetam (SV2AR Block - no glutamate release. Broad spectrum)
  3. Phenobarbital (Barbiturate. GABA-A R allosteric binding)
147
Q

Antipsychotics - 1st generation

A

Phenothiazines: Chlorpromazine (D2R, MRs, alphaR, H1R)
Butyrphenones: Haloperidol (D2R, MR, alphaR) & Droperidol (D2R, H1R)
Thioxanthene: Flupentixol (D2R, 5-HT, alphaR)

148
Q

Antipsychotics - 2nd Generation Atypical (5HT2A Blockade)

A
  1. Clozapine (MAIN: D2R blocker. MR, alphaR, 5HT R block)
  2. Olanzapine (5HT, D2R block)
  3. Risperidone (5HT R block. No MR block)
  4. Aripirazole (PARTIAL D2R & 5HTR agonist)
  5. Tiapride (D2/D3 R antagonist)
  6. Cariprazine (D2/D3R antagonist - hungarian drug)
149
Q

Bipolar Disorder treatment

A
  1. Lithium (Inhibit Inositol Monophosphatase - Decrease Gq, less Gs action)

Can add Carbamazepine & Valproate

150
Q

Lithium Side Effects

A
  1. Flu-like symptoms
  2. GI distress
  3. Hypothyroid
  4. Nephrogenic DI
  5. Acute toxicity
  6. Teratogen - Ebstein’s anomaly
151
Q

Tricyclic Antidepressants + Tetracyclic and Heterocyclic

A
  1. Clomipramine (TCA - Inhibit NET&SERT)
  2. Amitriptyline (TCA - Inhibit NET&SERT)
  3. Maprotiline (TetraCA - Inhibit NET more)
  4. Bupropion (HeteroCA - Inhibit DAT)
152
Q

Serotonin Antagonist Antidepressants

A

Trazodone (Post synaptic 5-HT2A Receptor antagonist & SERT)

153
Q

MAO Inhibitors

A
  1. Moclobemide (MAO-A - Antidepressant. Also inhibit Tyramine metabolism. Reversible)
  2. Selegiline (MAO-B - Parkinson treatment)
154
Q

SSRIs

A
  • Inhibit presynaptic reuptake of 5-HT*
    1. Fluocetine (long T1/2)
    2. Citalopram 1x20mg
    3. Sertaline

1st line of treatment for depression & anxiety

155
Q

SNRIs

A
  • Inhibit NET & SERT. No cholinergic/adrenergic effect*
    1. Venlafaxine (Panic, OCD, PTSD)
    2. Duloxetine (Diabetic neuropathy)
    3. Reboxetine (Selective NET)
156
Q

Atypical antidepressants

A
  1. Mirtazipine (alpha2R selective antagonist - Increase presynaptic release of NE& 5-HT)
  2. Agomelatine (MT1R agonist & 5HT2&3R inhibitor)
  3. Tianeptine (GABA-R modulator, D2/3 R agonist, 5HT-R inhibitor)
157
Q

Benzodiazepines

A

*Potentiate GABA by allosterically binding on GABA-A Receptor. Rely on endogenous GABA)
1. Nitrazepam, Midazolam (short acting)
2. Alprazolam (intermediate) 2-3×0,25-0,5mg
3. Diazepam (long acting): 5-10mg
In epileptiform seizures iv. 30mg
4. Clonazepam (long acting)

158
Q

Non-BZD hypnotics

A
  1. Zaleplon (GABAa-R binding)
  2. Zolpidem (GABAa-R binding)
  3. Melatonin (MT1&MT2 Rs at suprachiasmatic nucleus of hypothalamus) - Sleep ONSET
  4. Ramelteon (MT1&MT2 Rs) - sleep ONSET
159
Q

Non-BZD anxiolytics

A
  1. Buspirone (5-HT1 partial agonist)

2. SSRIs

160
Q

Barbiturates

A
  • Bind GABAaRs*
    1. Thiopental - Short acting, induction of IV anesthesia
    2. Phenobarbital - Long acting, Anticonvulsive (oral/IV)
161
Q

IV anesthetics for induction

A
  1. Thiopental
  2. Propofol
  3. Etomidate (Bind GABAaR)
  4. Fentanyl
  5. Dexmedetomidine (cental alpha2 agonist - for ICU patients)
162
Q

IV Anesthetics for maintenance

A
  1. Propofol (Potentiate Chloride current via binding GABAaR)

2. Fentanyl (opioid μ agonist)

163
Q

Dissociative Anesthesia IV anesthetic

A

Ketamine (Inhibit NMDA-R complex)

CV stimulation

164
Q

Conscious sedation IV anesthetic

A

Midazolam (antidote: Flumazenil)

165
Q

IV anesthetics causing CV & respiratory depression

A

Thiopental, Propofol, Midazolam, Fentanyl

166
Q

Inhaled anesthetics (Gas)

A

N2O

>100% MAC value

167
Q

Inhaled anesthetics (volatile liquids)

A
  1. Desflurane (MAC: 6.5%)
  2. Isoflurane (1.4%)
  3. Sevoflurane (2%)

NOTE: Skeletal m. hypersensitivity => Malignant hyperthermia. Give Dantrolene

168
Q

Narrow spectum, beta lactamase SENSITIVE

A
  1. Penicillin G (IV)
  2. Penicillin V (oral)
  3. Benzathine Penicillin G (IM depot shot)
169
Q

Narrow spectrum, beta lactamase RESISTANT

A
  1. Nafcillin (IV)
  2. Oxacillin
    * Do not cover MRSA*
170
Q

Broad spectrum, beta lactamase SENSITIVE

A
  1. Ampicillin (IV)

2. Amoxicillin (pos) 3×500-1000mg

171
Q

Extended spectrum, beta lactamase SENSITIVE

A

Piperacillin (IV)

172
Q

Beta lactam combos

A
  1. Amoxicillin/ Clavulanic acid
  2. Ampicillin/Sulbactam
  3. Piperacillin/Tazobactam
173
Q

Cephalosporins 1st gen

A
  1. Cefazolin (surgical prophylaxis)
  2. Cephalexin

Gram + cocci

174
Q

Cephalosporins 2nd gen

A
  1. Cefoxitin
  2. Cefuroxime

Gram + cocci with gram - coverage

175
Q

Cephalosporins 3rd gen

A
  1. Ceftriaxone (hospital acquired pneumonia & single IM dose for gonorrhea)
  2. Cefotaxime
  3. Cefixime
  4. Ceftazidime (pseudomonas)

Gram - increased coverage

176
Q

Cephalosporins 4th gen

A

Cefepime (broad spectrum, beta lactamase resistant)

Pseudomonas!

177
Q

Cephalosporins 5th gen

A
  1. Ceftaroline fosamil
  2. Ceftalozane/tazobactam

TREAT MRSA!

178
Q

Probenecid inhibits tubular secretion of _____

A
  1. Cephalosporins
  2. Penicillin
  3. Methotrexate
179
Q

Monobactam

A

Aztreonam
MOA: Bind PBP-3 ONLY in Gram- bacteria
(Klebsiella, Pseudo, Serratia)

180
Q

Carbapenems (2nd gen)

A
  1. Imipenem (decrease seizure threshold)
  2. Meropenem

*Reserve Antibiotics, Pseudomonas. Resistant to most beta lactamases

181
Q

Glycopeptide Antibiotics

A

MOA: Bind D-Ala-D-Ala, inhibit transglycosylation. BACTERICIDAL. Parenteral

  1. Vancomycin
  2. Teicoplanin
  3. Ortivancin
182
Q

Lipopeptide antibiotics

A

MOA: Irreversibly inserts into cytoplasmic membrane, disrupt gradient. BACTERICIDAL

Daptomycin (MRSA, VRSA, VRE)

NOTE: causes rhabdomyolysis, be careful if patient takes statins too

183
Q

Polypeptide Antibiotics

A

MOA: Inhibit peptidoglycan precursos translocation. Bactericidal/ Bacteriostatic

Bacitracin (topical due to severe nephrotoxicity)

184
Q

Tetracyclines

A

MOA: Bind 30S. Bacteriostatic. Chelators (Ca, Fe, Mg). Accumulate in teeth - teratogen

  1. Tetracycline (pos)
  2. Doxycycline: first day 200 mg, than 100 mg 1x daily
  3. Tigecycline (IV only) - Glycylcycline
185
Q

Aminoglycosides

A

MOA: Bind 30S, Needs O2 to penetrate cell wall (combine with beta lactams). Inhibit initiation complex, induces misreading of mRNA & inhibit translocation => Bactericidal

  1. Gentamycin - Tobramycin -Amikacin -Netilmicin
  2. Streptomycin (combine with penicillin)
  3. Neomycin - Kanamycin (Topical. Orally- remains active in GI tract)
186
Q

Chloramphenicol

A

MOA: Reversible binding of 50S. Bacteriostatic
Used as a topical treatment due to toxicity
Empirical treatment of bacterial meningitis

CYP450 Inhibitor. Suppress RBC production. Grey baby syndrome

187
Q

Oxazolidones

A

Linezolid

MOA: Bind 50S. Inhibit initiation complex for translation. Bacteriostatic
Inhibit MAO-A & B
MRSA, PRSP, VRE

188
Q

Macrolides

A

MOA: Bind 50S. Bacteriostatic

  1. Erythromycin (txt walking pneumonia). Inhibit CYP450
  2. Roxithomycin (no activity against MRSA & PRSP). Inhibit CYP450
  3. Azithromycin 1x500mg for 3 days
  4. Clarithromycin. CYP450 Inhibitor
189
Q

Ketolides

A

MOA: Similar to macrolides, especially erithromycin

Telithromycin (use for macrolide-resistant strains. CYP450 Inhibitor)

190
Q

Clindamycin

A

MOA: Bind 50S. Bacteriostatic
Narrow spectrum. For Gram+ due to poor penetration of Gram - outer membrane.

NOTE: Can have C.difficile superinfection!

191
Q

Streptogramin

A

MOA: Bind 50S - block exit channel on ribosome. Bactericidal

  1. Quinupristin
  2. Dalfopristin

Reserve antibiotics. CYP450 Inhibitor

192
Q

Antimetabolite (antifolate) antibiotics

A
  1. Sulfonamides (Inhibit DHP synthase)
  2. Trimethoprim (DHF reductase inhibitor)
  3. Pyrimethamine/Sulfadiazine (Txt for toxoplasmosis)
  4. Proguanil (malaria prophylaxis)

TMP-SMX combo is bactericidal

193
Q

Fluoroquinolones (-floxacin)

A

MOA: Inhibit DNA gyrase (topoisomerase II) in Gram - and Topoisomerase IV in Gram+
Bactericidal. Post Antibiotic effect

  1. Norfloxacin/ Ciprofloxacin/ Ofloxacin (2nd gen)
  2. Levofloxacin (3rd gen) - Respiratory walking pneumonia
  3. Moxifloxacin (4th gen)
194
Q

Metronidazole

A

MOA: Forms free radicals
Bacteridical. High CSF concentration
CYP450 Inhibitor
Also used to treat protozoal diseases

195
Q

Fidaxomicin

A

MOA: Inhibit bacterial RNA pol. Oral
Bacteridical
Can txt C.difficile

196
Q

Rifaximin

A

MOA: Inhibit DNA-dep RNA pol
Rifampicin derivative
Use in Hepatic encephalopathy

197
Q

Mupirocin

A

MOA: Inhibit bacterial protein synthesis by binding isoleucyl tRNA synthetase
Topical (not absorbed)

198
Q

Fusidic acid

A

MOA: Inhibit bacterial elongation factor G
Bacteriostatic
Topical for skin infections & Oral for MRSA

199
Q

Polymyxin E

A

MOA: cationic detergent. Bactericidal

200
Q

Fosfomycin

A

MOA: Inhibit enolpyruvate transferase -> No N-acetylglucosamine (cell wall precursor)
Bactericidal

201
Q

Nitrofurantoin

A

Urinary antiseptic

No systemic antibacterial effects

202
Q

TB 1st line treatment

A
  1. Isoniazid (inhibit mycolic acid synthesis-Bactericidal -CYP450 Inhibitor)
  2. Rifampin (Inhibit DNA-dep. RNA pol - Bactericidal)
  3. Ethambutol (cell-wall synthesis inhibitor)
  4. Pyrazinamide (no known MOA. bacteriostatic)

RIPE - Phase I: 2 months
Phase II: 4-7 mo. Rifampin & Isoniazid

203
Q

TB 2nd line

A
  1. Streptomycin/ Amikacin/ Kanamycin

2. Cycloserine (inhibit peptidoglycan synthesis)

204
Q

Leprosy treatment

A
  1. Dapsone ( Inhibit folic acid synthesis - Bacteriostatic)

2. Rifampin

205
Q

Antiherpetic agents

A
  1. Acyclovir (Inhibit viral DNA pol - HSV1/2, VZV & IV for HSV encephalitis)
  2. Valaciclovir/Famciclovir (Inhibit viral DNA pol - VZV & acyclovir resistant strains)
  3. Ganciclovir (Inhibit viral DNA pol - 1st line for CMV)
  4. Valganciclovir (ganciclovir prodrug with better oral bioavailability)
  5. Cidofovir (Inhibit Viral DNA pol - HSV, CMV, HPV, Adenovirus & TK- strains. IV)
  6. Foscarnet (not an antimetabolite - Inhibit both RNA&DNA pol - CMV 2nd line agent. IV)
206
Q

Antiretrovirals - NRTIs

A

MOA: Prodrugs. Inhibit binding of nucleosides to reverse transcriptase

  1. Zidovudine - Pregnancy safe
  2. Lamivudine - also used for Hep B
  3. Emtricitabine - CI in pregnancy/child/ renal&hepatic Failure
  4. Abacavir
  5. Tenofovir - also used for Hep B. No phosphorylation needed for activation
  6. Stavudine (do not use with zidovudine)
  7. Didanosine - dose dependent pancreatitis
  8. Zalcitabine
207
Q

Antiretrovirals - NNRTIs

A

MOA: Bind on reverser transcriptase (diff site from NRTIs). No phosphorylation needed.
Not active against HIV-2

  1. Etravirine (Inhibitor + Inducer of CYP450)
  2. Nevirapine (CYP450 Inducer) - Used to prevent vertical transmission
  3. Efavirenz (TERATOGENIC)
  4. Delavirdine (Teratogenic)
208
Q

Antiretrovirals - Protease Inhibitors, Integrase inhibitors & entry inhibitors

A
  1. Maraviroc (Blocks CCR5 receptor so no interaction b/w viral gp120 and CD4 on lymphocytes)
  2. Elvitegravir (Bind integrase so viral DNA cannot integrate in host DNA)
  3. Ritonavir (PI - most common. MOST POTENT CYP450 INHIBITOR)
  4. Lopinavir (PI - use with ritonavir)

NOTE: Ritonavir is often added to HIV txt to increase serum levels of other antivirals due to CYP450 inhibition

209
Q

Anti-influenza

A
  1. Amantadine/ Rimantidine (Inhibit M2 protein needed for onset of infection)
  2. Oseltamivir/ Zanamivir (inhibit neuramidase - no new virion clumping)
210
Q

Anti-RSV

A
  1. Palivizumab (Human monoclonal Ab - no fusion)

2. Ribavirin

211
Q

Hepatitis antivirals (non specific)

A
  1. IFN-α (activate cytokines, increase JAK-STAT path)
  2. Entecavir (guanosine analogue - Inhibit HBV DNA pol)
  3. Tenofovir (NRTI)
  4. Ribavirin ( Guanosine analogue, Inhibit IMP DH so no GMP. No Viral RNA pol)
212
Q

Uses of IFN-α

A

Hep B, HHV-8, Hairy cell leukemia, malignant melanoma, papillomatosis, RCC, HPV

213
Q

Hepatitis antivirals (DAAs)

A
  1. Paritaprevir/ Grazoprevir (PI - NS3/4A)
  2. Sofosbuvir (NPI - NS5B)
  3. Dasabuvir (NNPI - NS5B)
  4. Velpatasvir/ Elbasvir (NS5A)
214
Q

Malaria drugs

A
  1. Chloroquine (Inhibit heme polymerization) + Hydroxychloroquine (less toxic and for AI)
  2. Mefloquine (Unknown MOA - blood schizontocide)
  3. Quinine (Inhibit protozoal DNA replication - schizontocide)
  4. Artemether (Produce free radicals - schizontocide)
  5. Lumefantrine (Unknown MOA)
  6. Malarone= Proguanil (Inhibit DHFR Thimydylate synthase) + Atovaquone (disrupt mitochondrial metabolism)
  7. Primaquine (Tissue schizonticide - oxidants)
215
Q

Helminthic infections

A
  1. Mebendazole (Inhibit MT synthesis & glucose uptake)
  2. Ivermectin (Facilitate GABA-med. transmission thus immobilized parasites due to hyperpolarization)
  3. Niclosamide (Uncouple oxidative phosphorylation)
216
Q

Antifungal agents

A
  1. Amphotericin B (Form pores in fungal membrane by interacting w/ ergosterol. Fungicidal)
  2. Nystatin (same as amphotericin but only TOPICAL due to toxicity)
  3. Clotrimazole (Imidazole. Topical, OTC. Interfere with ergosterol synthesis. CYP450 Inhibitor)
  4. Fluconazole (1st gen Triazole. Cross BBB so can txt Cryptococcus meningitidis. Interfere w/ ergosterol synthesis. CYP450 Inhibitor)
  5. Itraconazole ( 1st gen Triazole. CYP450 Inhibitor)
  6. Voriconazole (2nd gen Triazole, for Aspergillus. Cause Visual disturbances. CYP450 Inhibitor.)
  7. Flucytosine (5-FU, Incorporate into fungal RNA & Inhibit thimidylate synthase. Antimetabolite)
  8. Caspofungin (Echinocandin. Inhibit synthesis of beta(1,3) glucan of fungal cell wall
  9. Terbinafine (Inhibit squalene epoxidase - fungal membrane)
217
Q

Disinfectants & Antiseptics

A

Alcohols: Ethanol 70%, Isopropyl alcohol 70-90%
Halogens: Povidone-iodine
Oxidizing agents: H202
Chlorinated phenols: Chlorhexidine
Cationic surfactant: Octenidin, Invert soaps

Pharmacology Final (1 decks)

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