Drug Classes&Names Flashcards
Bronchodilators (COPD and Asthma Treatment)
- beta2 selective agonists
- Leukotriene Inhibitors
- Methylxanthines
- Muscarinic Antagonists
- Antihistamines (mast cell stabilizers)
- Anti-IgE Ab (Omalizumab)
- Corticosteroids
Beta2 selective agonists
-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
Muscarinic antagonists (for bronchodilation)
- Ipratropium
- Tiotropiuum
MOA: M3R inhibitor (Gq-coupled)-> Prevent bronchoconstriction by vagal discharge
Methylxanthines
Theophylline
MOA: PDE Inhibition-> Increased cAMP-> Bronchodilation, decreased inflammation. CYP450!!
Corticosteroids (for bronchodilation)
- Budesonide, Dexamethasone
- Prednisolone
MOA: Inhibit PLA2 -> Decrease COX-> Less inflammatory mediators
Leukotriene antagonists
Montelukast
MOA: Inhibit LT synthesis/action-> Less inflammation + less bronchoconstriction
Antihistamines (Mast cell stabilizers - bronchodilation)
Cromolyn (not in excel sheet but important)
MOA: Prevent degranulation of mast cells
Anti-IgE antibody
Omalizumab
MOA: Bind Fc portion of IgE Abs -> cannot bind to mast cells -> no inflammatory response
Cough medication
- Antitussive agents (non-productive cough)
2. Muco-active (productive cough) - Expectorants& Mucolytics
Antitussive agents
- Codeine (Opioid)
MOA: μ-Receptor agonist. Suppress cough reflex - Butamirate (Non-opioid) & Prenoxidiazine
MOA: Centrally acting - Suppress cough reflex. Peripheral -> Bronchodilation, suppress inflammation
Muco-active Drugs
- Mucolytics:
Bromhexine (MOA: Increase serous fluid production)
Acetylcysteine (MOA: Decrease disulfide bonds in mucus, decrease viscosity) - Expectorants
Peripheral Vascular Disease drugs
- General - Statins, Aspirin/Clopidogrel, Anti-HTN, ACE Inhibitors/ARBs (1st line of treatment)
- Cilostazol (PDE-3 Inhibitor, Vasodilation)
- Pentoxifyllin (Reduce blood viscosity)
- Vinpocetin (Inhibit Na &Ca channels, increase cerebral perfusion)
- Nicergoline (α1 antagonist, Cholinergic function, decrease platelet aggregation, increase metabolism, neurotrophic & antioxidant)
- Ca-Dobesilate (Reduce microvascular permeability)
Migraine Treatment
- Acute Attack Therapy
2. Prophylactic Therapy (>4 attacks/month, severe attacks, >72hrs)
Acute Migraine Attack Therapy
- Non-specific:
Acetaminophen, Aspirin, caffeine, NSAIDs, Metoclopramide, Droperidol - Migraine specific:
Sumatriptan (MOA: 5-HT1D/1B agonist, Vasoconstriction, Decreased NP release, brainstem to inhibit pain pathway)
Ergotamine (MOA: Partial 5-HT2& αAR agonist)
Migraine Prophylactic Therapy
- Galcanezumab (MOA: CGRP antagonist-Vasoconstriction. Minoclonal Ab)
- Cinnarizine (MOA: Anti-histamine, Ca-channel blocker)
- Propanolol (MOA: β-non selective antagonist)
- Verapamil (MOA: Ca-ch. blocker, Non-DHIP)
- Carbamazepin (MOA: Inhibit voltage-gated Na ch, less glutamate release)
- Valproic acid (MOA: Inhibit high-freq. firing, Inhibitory actions of GABA)
- Imipramine (MOA: inhibit 5-HT &NE reupate - Tricylic antidepressant) CYP450!!
ACE Inhibitors
-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
ARBs
-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
Heart Failure Treatment (Decrease load on heart)
- ACE Inhibitors/ ARBs
- Diuretics (Thiazides, Loop, K+ Sparing agents)
- Beta blockers
- Vasodilators (isosorbide dinitrate, hydralazine,NO)
- PDE Inhibitors (Milrinone, Theophylline) - For AHF
- Neprilysin inhibitors (Sacubitril) - For CHF
- Ca-sensitizing agents (Levosimendan) - For AHF
Heart Failure Treatment (Positive Inotropic agents)
Digoxin (maintenance dose 1×0,25mg)
Acute Heart Failure Treatment
- beta agonists (Dobutamine & Dopamine)
- diuretics (MRAs, Acetazolamide)
- vasodilators (Isoborbide dinitrate, hydralazine)
- PDE Inhibitors (Milrinone, Theophylline)
- ACE Inh/ARBs
- Calcium sensitizers (levosimendan)
Chronic Heart Failure Treatment
- Digoxin
- Diuretics
- Beta blockers
- ACE-Inhibitors/ARBs
Digoxin MOA
- 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
Types of Diuretics
- Carbonic anhydrase inhibitors
- Osmotic diuretics (aquaretics)
- Loop Diuretics
- Thiazides
- K+ - Sparing
- SGLT-2 antagonists (not used as a diuretic but will increase urine volume)
- Drugs affecting ADH (ADH antagonists)
Carbonic Anhydrase Inhibitors
Acetazolamide
MOA: Inhibit Carbonic Anhydrase, HCO3- stays in lumen, less H20 reabsorbed in tubule
SOA: Proximal convoluted Tubule
Note: SULFA DRUG (watch for allergies)
Osmotic Diuretics (Aquaretic)
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
Loop Diuretics
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
Loop Diuretics Side effects & CI
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)
Thiazide diuretics
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
Thiazide diuretics SE & CI
SE: HyperGLUC
Contraction alkalosis, hyponatremia, hyperGlycemia, hyperLipidemia, hyperUricemia, hyperCalcemia, sulfa allergy
CI: Digoxin (electrolyte imbalances), DM pts (decrease Insulin release by opening K+ channels)
K+ - sparing diuretics
- Aldosterone receptor Inhibitors (MRA): Spironolactone, Eplerone
- ENaC Inhibitors (Amiloride)
SOA: Collecting duct (principal& intercalated cells)
Aldosterone R. Inhibitors Uses
- Hyperaldosteronism (Conn’s Sy)
- Hypokalemia from other diuretics
- Congestive HF (inhibits cardiac remodelling)
- Antiandrogenic use (inhibit 17alpha hydroxylase -PCOS, Female hirutism)
ENac Inhibitor Uses
- Hypokalemia
- NDI
- Liddle’s sy. (too many ENaCs)
Which channels do Aldosterone Receptor Inhibitors affect?
- Na+/K+ ATPase
- ENaC
- K+ channels on apical membrane
- H+ ATPase (intercalated cell)
ADH antagonists (MOA, SOA, SE)
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
Types of Antiarrhythmic drugs
- Class I - Na+ channel blockers (Rhythm control)
- Class II - beta blockers (Rate control)
- Class III - K+ channel Blockers (Rhythm control)
- Class IV - Ca channel blockers (Rate control)
- Class V - Others (adenosine, Mg2+, K+, Digoxin - Rate control)
Class I antiarrhythmics
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
Class II antiarrhythmics
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
Class III Antiarrhythmics
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
Amiodarone Side Effects
- Lung fibrosis - Restrictive Lung disease
- Hepatotoxicity - Hypersensitivity Hepatitis
- Hypo/Hyperthyroidism
- Blue/Gray deposits on cornea/skin
- Photodermatitis
- AV Block
- Torsades
- Inhibit CYP450 so interfere with other CYP450 drugs
- Induce Heart Failure
Class IV Antiarrhythmics
Verapamil
MOA: Inhibit Ca channels, slow down phase 0 and phase 4 - Rate control + Decrease cardiac contractility and BP
Class V Antiarrhythmics
- Adenosine: A1R activation -> hyperpolarization-> inhibit Ca channels. 1st line agent for acute supraventricular tachys
- Digoxin: Direct stimulation of vagus nerve
- K+
- Mg2+ : can treat torsades and digoxin toxicity
Order of treatment for Rate control of AF
1st line: Class II or Class IV
2nd line: Digoxin
Hypertensive Treatment
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
Types of Antihypertensives
- Diuretics (Thiazides/ Loop)
- Sympatholytics
- Vasodilators
- RAAS system drugs
HTN emergency management
All drugs are given IV.
- Beta blockers (esmolol)
- Ca ch. blockers (Nicardipine)
- Nitroprusside
- Hydralazine
- ACE Inhibitors (captopril)
Ca channel Inhibitors
MOA: Inhibit L-Type Ca channels in smooth muscle cells (vessels) and on heart
- Dihydropyridine (DHP) - more vascular effect
- Non-dihydropyridines - more cardiac effect
DHPs (names, uses, SE)
- 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
Non-DHPs (names, uses, SE)
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
Vasodilating drugs for HTN treatment (Not CCB)
- Nitric Oxide releasing agents (Hydralazine)
- Endothelin antagonists (Bosentan)
- PDE-5 Inhibitors (Sildenafil)
RAAS pathway drugs as antihypertensives
- ACE Inhibitors (Captopril, Enalapril, Perindopril, Ramipril)
- ARBs (Losartan, Valsartan in combo w/ Sacubitril - ARNi, Irbesartan)
- MRAs (Spironolactone, Eplerenone)
Angina pectoris (Ischemic Heart Disease) drug treatment
- Nitrates (nitroglycerin - 0.5mg sublingual & isosorbide dinitrate)
- Ca channel blockers (Nifedipine, Verapamil)
- Beta blockers (Propanolol)
- Trimetazidine (MOA: partial fatty acid oxidation inhibition - pathway goes into glucose oxidation, less O2 consumption, optimize cellular energy processes)
- Ivabradine (MOA: Inhibit If Na channels in SA node-> Hyperpolarization-> Lower HR -> Decreased O2 demands)
Nitrates SEs and CIs
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
Dyslipidaemia Drugs
- Statins
- Bile acid sequestrants-Resins
- Sterol absorption inhibitors
- Fibrates
(not in topic list but 5. Niacin and 6. Others eg Folic acid)
Statins
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
Bile acid sequestrants - resins
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
Sterol Absorption Inhibitors
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
Fibrates
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
Histamine actions
- Type I allergic rxn (IgE mediated)
- Increase Vascular permeability
- Bronchial muscle constriction
- Increase Nasal&Bronchial mucous production
- Neurotransmitter (mediate sleep/arousal)
Antihistamine drugs
H1R antagonists (1st & 2nd gen)
1st generation H1R antagonists
- Diphenhydramine
- Promethazine (more sedative/autonomic effects)
- 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)
2nd generation H1R antagonists
- Cetirizine
- Loratadine
- 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
Cholinergic Transmission NT and Receptors
NT: Acetylcholine
Receptors: Nicotinic and Muscarinic (Sympathetic and Parasympathetic postganglionic fibers)
Cholinomimetics
- Carbachol (MR &NR) - open angle glaucoma
2. Pilocarpine (MR) - closed angle glaucoma, xerostomia
Anticholinesterases (Indirect agonists)
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)
Antimuscarinics
MOA: Reversible block. Block Parasympathetic activation
- Atropine (M3R-Eye & M2R-Heart): mydriasis, increase HR & AV conduction. Dose 0,3-1,0mg
- Ipratropium, Tiotropium (M3R-Lung): Bronchodilation
- Oxybutynin, Solifenacin (M3R-Genitourinary): Reduce urinary incontinence
- Scopolamine(transdermal), Butyl-scopolamine(oral): M1R-CNS, Motion Sickness
- Cyclopentolate (M3R-Eye): Cycloplegia
- Procyclidine (M1R-CNS): Parkinson’s
Catelcholamines
- Epinephrine (β2&αRs dose dependent) - Anaphylactic shock - sc. or im. 0,15-0,5mg, iv. 0,05-0,1mg
resuscitation 1mg - Norepinephrine (α1>α2, β1) - Septic Shock
- Isoprenaline (β1= β2) - Cardiac arrest, complete heart block
- Dobutamine (β1> β2) - Cardiogenic shock
- Dopamine (indirect. D1R, β1 @low dose. D2R @high dose) - increase CNS activity, Increase renal blood flow
Indirect sympathomimetics
Ephedrine (Decongestant, HypoTN, stimulant)
MOA: Displace stored catelcholamines from nerve endings
Phenylephrine (HypoTN, Rhinitis, ischemic priapism)
Selective α2 agonists
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
α-Receptor antagonists
- Non-selective : Phentolamine - Pheochromocytoma pre-op, Antidote for HTN due to α-agonist OD
SE: Orthostatic hypoTN - α1-selective: Prazosin, Doxazosin, Tamsulosin - HTN, BPH, Prazosin for PTSD
SE: Orthostatic hypoTN - α2, α1,β: Urapidil + 5-HT weak agonist - HTN, BPH
- Both α &β: Carvedilol - HTN Emergency, decrease variceal bleeding, decrease mortality in HF
β-Receptor antagonists
- 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) - β1 selective - cardioselective
- Metoprolol ( 2×25-100mg) , Bisoprolol, Nebivolol (HTN, CHF, Angina, Anti-arrhythmics Class II, ACS)
- Esmolol (IV, HTN Emergency, thyroid-storm arrhythmias) - β&α combined
- Carvedilol (CHF, Reduce mortality)
Centrally acting Skeletal muscle relaxants (Spasmolytics)
- Baclofen: GABA-b. Cerebral palsy, MS. SE: Sedation, rebound plasticity
- Diazepam: GABA-a. Chronic&Acute spasm. SE: CNS depressant, tolerance & dependence
- Tizanidine: α2 agonist. MS, Stroke. SE: sedation, hypoTN, rebound HTN
- Tolperisone: Na+ & Ca+ ch blocker. Acute spasm. SE: Strong antimuscarinic effects
Direct acting muscle relaxants
- Dentrolene
MOA: RyR1 antagonist -> block Ca+ release in SR -> less actin-myosin interaction
Use: Malignant Hyperthermia. SE: Hepatotoxic - Botulinum toxin
MOA: inhibit SNARE to prevent synaptic exocytosis -> Flaccid paralysis
Use: spasm, migraine, cosmetics, hyperhidrosis
Skeletal Muscle Relaxants acting on the NMJ
- Non depolarizing - competitive antagonists at sk muscle nAchRs (Nm) aka. Curare type
- Depolarizing - agonist at Nm, can stimulate ganglionic nAchR and cardiac M3R
Non-depolarizing NMJ anesthetics
- Mivacurium - short acting. Pseudocholinesterase
- Rocuronium - IM acting. hepatic metabolism
- Cisatracurium - IM acting. spontaneous metabolism.
- Atracurium - IM acting. spontaneous.
- Piperacurium - long acting. renal metabolism
SE: Histamine release (HypoTN), Prolonged apnea, Tachy
Depolarizing NMJ Anesthetics
Succinylcholine (Suxamethonium)
Parenteral with 5-10 min duration. metabolized by cholinesterase enzymes
Use: Surgery with brief duration, Status epilepticus
SE: Arrhythmias, malignant hyperthermia
Types of local anesthetics
- Amides
- Esters
Order of nerve blockade: A delta, C, A beta (prefer small, myelinated nerve fibers)
Amide local anesthetics
- Lidocaine (short acting) - CYP450 drug
- Articaine (short acting, most rapid onset of all LA)
- Bupivacaine (longest acting, most potent, CNS toxicity, CYP450 drug)
Ester Local anesthetics
- Cocaine
Surface acting, metabolized by pseudocholinesterase, only LA that’s vasoconstricting
Glucocorticoids (-sone suffix)
parenteral & oral
- Hydrocortisone - short acting, replacement therapy in adrenal insufficiency
- Prednisolone - IM acting
- Methylprednisolone - IM acting (4-250 mg)
- Triamcinolone - IM acting. Usually topical. High toxicity compared to others
- Dexamethasone - Long acting
Topical Glucocorticoids
- Fluocinolone
- Budesonide
- Mometasone
- Fluticasone
Mineralocorticoids
- Aldosterone (endogenous)
2. Fludrocortisone
Corticosteroid Antagonists
- MRA antagonists (spironolocatone& eplerone)
2. Metyrapone (11 beta hydroxylase inhibition)
Androgens
- Testosterone-undecanoate (testosterone analogue)
- Nandolon (anabolic steroid)
- Bicalutamide (Testosterone Receptor Inhibitor)
- Finasteride (5alpha reductase inhibitor)
- Goserelin (GnRH analogue)
- Degarelix (GnRH antagonist)
- Sildenafil (PDE-5 Inhibitor, Help with Erectile dysfunction)
Estrogens and Antiestrogens
- Ethinyl-estradiol (CYP450 metabolism)
- Estradiol
- Tamoxifen (SERM, Hormone-responsive breast cancer)
- Raloxifen (SERM, Osteoporosis in post-menopausal women)
- Clomifene (SERM, ovulation induction)
- Anastrozole (Synthesis Inhibitor-Aromatase, Hormone Responsive breast cancer adjuvant)
- Goserelin (GnRH analogue, Ovarian suppression, central precocious puberty)
- Degarelix (GnRh antagonist, Controlled ovarian stimulation)
How SERM (Selective Estrogen Receptor Modulators) work
Estrogen antagonist @ breast, CNS, uterus
Estrogen agonist @liver, bone
Progestins
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
Antiprogestins
- Mifepristone (Glucocorticoid&Progesteron R antagonist)
Medical abortion in combo with PGE analogue - Ulipristal acetate (SPRM)
Day after pill, myoma growth suppression
Oral Hormonal Contraceptives
- Combined: Ethinyl Estradiol + Progestin (Levonorgestrel, Desogestrel, Dosperidone)
- Minipill (progestin only)
Other contraceptives
- Depot Injection - Medrocyprogesterone-acetate
2. IUD -levonorgestrel
Thyroid and antithyroid drugs
- Levothyroxine (T4) - give in hypothyroidism (25-150 µg)
- Propythiouracil (PTU) - inhibit TPO and 5’ deiodinase (hyperthyroidism)
- Methimazole (Thiamazole) - inhibit TPO
How to treat thyroid storm (untreated hyperthyroidism)
- Beta blockers (propanolol) - treat SNS effects
- PTU/Methimazole - decrease T3&T4 levels
- Glucocorticoids (hydrocortisone) - treat opthalmopathy
- KI
All given IV. PTU & Methimazole given bolus IV
Anterior Pituitary Hormone Drugs
GH antagonist:
Octreotide - Inhibit release of GH, Insulin, Glucacon, Gastrin
Prolactin antagonist:
Bromocriptine - D2R agonist, inhibit pituitary secretion of prolactin
Posterior Pituitary Hormone Drugs
- Oxytocin - Oxytocin receptor agonist. Increase uterine contractions & induce labor/ control uterine hemorrhage
- Desmopressin - ADH agonist (V2R). Treat Nephrogenic DI, Haemophilia A & VWF Disease
Anticoagulant drugs types
1. Heparin MOA: Inhibit formation of fibrin clots. Bind ATIII, inhibit factors IX, XI, XII & Plasmin 2. Direct acting thrombin inhibitors 3. Direct acting Factor Xa inhibitors 4. Coumarin - Warfarin
Heparin drugs
- Unfractionated heparin (highest chance of HIT. use for DVT, PE, acute MI)
- Dalteparin - Low molecular weight heparin (watch out for renal insufficiency)
- Fondaparinux (high specificity to factor Xa)
REVERSE: Protamine Sulfate
Direct acting thrombin inhibitors
- Bivalirudin (anticoagulation in pts with HIT. Give with aspirin during PCI)
- Dabigatran-etexilate (chronic therapy for AF to prevent clot formation)
Direct acting factor Xa inhibitors
Rivaroxiban (prevent venous thromboembolism post-op, prevent stroke in AF)
Warfarin uses
CHRONIC anticoagulation (AF, Thrombi, VTE, Post-Mi, heart valve damage)
CYP450 DRUG!
REVERSE: Vitamin K, FFP, PCC
Antiplatelet drugs
- COX inhibitors (Acetylsalicylic acid)
- Glycoprotein IIb/IIIa Inhibitors (Abciximab)
- ADP-R antagonists (clopidogrel, prasugrel, ticagrelor)
Fibrinolytics (-teplase)
- Alteplase
- 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
Bleeding Disorder Drugs
- 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
Anemia drugs
- Iron - Iron hydroxylide Polymaltose Complex
- Vitamin B12 (cobalamin)
- Folic acid (Vitamin B9)
- Epoetin alpha
- Filgrastim
Parenteral drugs for IDDM
- Insulin Lispro (Rapid acting)
- Regular Insulin (short acting)
- NPH-Insulin (IM acting) - combo w/ short acting
- Insulin Glargine (long acting)
- Liraglutide (GLP-1 analogue)
Oral antidiabetics
- Insulin secretagogues:
a) Sulfonylureas (2nd gen - Glimepiride, Glipizide)
b) Meglitines: Repaglinide - Biguanides: Metformin (2-3×500-850mg)
- DPP-4 Inhibitor: Vidagliptin
- SLGT-2 Inhibitors: Dapagliflozin
- alpha-glucosidase Inhibitora: Acarbose
Agents affecting bone mineral homeostasis
- Teriparatide - PTH analogue
- Cholecalciferol - Vitamin D3
- Raloxifene - SERM
- Alendronate & Zoledronate - Bisphosphonates
- Denosumab - IgG Ab
- Calcitonin
1st line treatment in osteoporosis
Bisphosphonates
Osteoporosis pharmacotherapy - Inhibit Bone resorption
- Hormone Replacement therapy
- SERM
- Bisphosphonates
- RANK-L Inhibitors
- Calcitonin analogues
Osteoporosis pharmacotherapy - Increase bone formation
- Teraparatide
- Ca2+ supplements
- vitamin D supplements
- Thiazides diuretics
Autoimmne Disease Drugs
- Cyclophosphamide (Alkylating agent)
- Methotrexate (Folate antimetabolite. Inhibit DHF reductase. S-phase)
- Leflunomide (Inhibit de novo pyrimidine synthesis)
- Azathioprin (-> 6-MP. Inhibit conversion of PRPP->IMP. No RNA/DNA synthesis. S phase)
- Mycophenolate - mofetil (IMP dehydrogenase. Less GMP, less WBC proliferation)
Cytokine gene expression & 5-ASA derivatives
- Cyclosporin A (bind cyclophilin, Calcineurin Inhibitor)
- Tacrolimus- FK506 (Bind FK-binding protein. Calcineurin inhibitor)
- Sirolimus (mTOR inhibitor)
- Tofacitinib (Inhibit JAK1&3)
- Sulfasalazine ( PPAR-γ agonist - Less TLRs&NFkB, Less cytokine, Inhibit COX&LOX. 5-ASA derivative)
Antibodies & Fusion Proteins
- ATG (Bind T-cells. Serum complement destruction)
- Rituximab (Anti-CD20. Monoclonal Chimeric)
- Infliximab (Anti-TNFa. Monoclonal Chimeric)
- Adalizumab (Anti-TNFa. Human)
- Tocilizumab (Anti-IL6 receptor)
- Ustekinumab (Anti-IL12&23)
- Natalizumab (Anti-integrin a4b1. Inhibit WBC entry via BBB)
- Dupilumab (Anti-IL4 Ra)
- Abatacept (fusion protein. CTLA-4 fusion protein, Bind CD80/86 on APC)
Chemo - Antimetabolites
- 5-Fluorouracil (Inhibit Thimydilate synthase) - combine with leucovorin for max effect
- Capecitavine (Bioactivated to 5-FU)
- Cytarabine (Inhibit DNA polymerase)
- 6-Mercaptopurine (Inhibit Purine Metabolism)
- Methotrexate ( Inhibit DHF Reductase)
- Pemetrexed (Folate antimetabolite)
Chemo - Alkylating agents
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
Chemo - Topoisomerase Inhibitors
- Etoposide (Inhibit Topoisomerase II) - G2 phase
- Irinotecan (Inhibit Topoisomerase I) - S phase
- Doxorubicin (antitumor antibiotic. Inhibit Topoisomerase II)
Chemo - Mitotic Spindle Inhibition
- Vincristine (vinca alkaloid, Inhibit MT polymerization)
- Docetaxel (Inhibit MT degradation so no mitotic spindle formation)
Both M-phase
Chemo - Hormonal agents
- Prednisolone (corticosteroid)
- Tamoxifen (SERM) - only one given to pre-menopausal women
- Anastrozole (Aromatase inhibitor)
- Goserelin (GnRH agonist - continuous)
- Degareliz (GnRH antagonist)
- Bicalutamide |(oral non-steroidal antiandrogen)
- Octreotide (Somatostatin analogue)
Chemo - Small molecules
- 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)
Chemo - large molecules
- 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)
Opioid analgesics - Natural
- Morphine - MorphineSO4 oral: 2×30-100mg, Morphine HCL iv: 10-20mg
- Codeine (anti-tussive)
Opioid analgesics - semisynthetic
- Hydromorphone (analgesia)
- Oxycodone (abuse)
- Dihydrocodeine (antitussive)
- Buprenorphine (withdrawal symptom management)
- Nalbuphine (spinal anesthesia)
Opioid μ analgesics - synthetic
- Fentanyl (transdermal/sublingual - anesthesia)
- Tramadol (chronic pain)
- Meperidine/Pethidine (analgesia in ER)
- Loperamide & Diphenoxylate (Anti-diarrheals - Loperamide has no CNS effects)
- Methadone (opioid withdrawal management)
Opioid antagonists
- Naloxone (IV. reverse opioid OD)
2. Methyl-naltrexone (Reduce nicotine and alcohol cravings + maintenance)
Gout drugs
- Colchicine (Inhibit MT assembly)
- Allopurinol (Xanthine Oxidase inhibitor)
- Rasburicase (Urate oxidase recombinant)
In acute gout attacks, give intraarticular steroids (prednisone)
Non-opioid analgesics (NSAIDs)
- Aspirin (acetylsalicilic acid - irreversible inhibition) dose dependent drug; For inhibiting the platelet aggregation 50-200mg
Analgesic and antipyretic dose 500mg) - Ibuprofen (pediatrics) 1-4×200-600mg
- Indomethacin (Acute gout attack. Closure Ductus Arteriosus)
- Naloxen (Acute gout. Dysmenorrhea)
- Diclofenac (MSK pain) 2-3x50mg
- Metamizole 500-1000mg
- Ketoprofen (-dex) (lower LTs)
- Phenylbutazine (Can cause aplastic anemia!)
- Meloxicam (more inhibition on COX-2)
- Celecoxib (Cox-2 selective)
- Acetaminophen (no peripheral COX inhibition)
1-4×500-1000mg
Acetaminophen toxicity antidote
N-acetylcysteine
Salicylate toxicities (OD)
Tinnitus, abdominal pain, fever, Double acid-base disorder (mixed)
Treat with Activated charcoal and IV NaHCO3
Antacids
- Mg (OH)2
- Al(OH)3
Decrease Warfarin & Tetracyclines absorption. Increase Quinidine absorption
Proton Pump Inhibitors
- Omeprazole (prodrug. Can inhibit clopidogrel activation)
2. Pantoprazole (oral and iv); ORAL: 2×20-40mg
H2Receptor inhibitors
Famotidine (decrease NOCTURNAL acid secretion) 2x20mg or 1x40mg
Laxatives
- Senna/ sennoside
- Bicasodyl
- Plant fiber
- MgSO4
- Lactulose
- Paraffin oil (pt must be upright when ingesting; avoid Lipoid pneumonia)
Antidiarrheals
- μ-opioid agonists in GI*
- Loperamide (no BBB cross)
- Diphenoxylate (Must combine with Atropine to avoid CNS effects)
- Activated charcoal
Antiemetics
- Diphenhydrinate (H1R blocker - combo of diphenhydramine&theophylline)
- Onsanserton (oral/IV) & Palonoserton (IV) - Inhibit 5HT3Rs in GI
- Metoclopramide (Inhibit D2Rs. Prokinetic at low dose, Antiemetic at high dose)
- Dropiredol (Inhibit D2Rs, antipsychotic)
- Aprepitant (Inhibit NK1R at area postrema) - CYP450 inhibitor
- Cannabinoid (agonist of CBRs, inhibit presyntaptic DA - AIDS wasting syndrome)
Abdominal & Urogenital painkillers /spasmolytics
smooth muscle drugs
- Butylscopolamine (Anticholinergic non-selective w/o CNS penetration)
- Solifenacin & Oxybutynin (M3R inhibitors. transdermal patch)
- Papaverine (CCB, inhibit PDE. Oral/IV)
Tocolytics (Smooth muscle drugs)
- Atosiban (Oxytocin R antagonist - IV)
- Terbutaline ( SABA - IV/pos)
- MgSO4 (IV - also used to prevent seizures in preeclampsia)
- Ethanol (IV)
Uterine contractants (Smooth muscle drugs)
- Oxytocin (Oxytocin R agonist - IV/intranasal)
- Ergotamine (Vasoconstrictor- alphaR agonist &partial @ 5TH2, Ergot alkaloid - IV)
NOTE: DO NOT GIVE BEFORE PLACENTA DELIVERY - Misoprostol (PGE1 analogue - Oral)
Note: combined with Mifepristone for abortion
BPH Smooth muscle drugs
Tamsulosin (uroselective alpha1 blocker - oral)
Liver & Biliary tract drugs
- N-acetylcysteine - acetaminophen toxicity/mucolytic
- Ursodiol (Decrease cholesterol absorption - CI: Acute hepatitis & biliary obstruction!!)
- Silimarin (antidote to amanita phalloides - support liver function)
Alzheimer’s drugs
- Rivastigmine (Cholinesterase inhibitor, tertiary, cross BBB)
- Memantine (NMDA-R Blocker)
Nootropic - Piracetam (cognition enhancer)
Parkinson’s drugs (precursors and endogenous release)
- Levodopa (DA precursor) - do not give in psychosis
- Carbidopa (DA DC inhibitor) combined with Levidopa
- Amantadine (Potentiate endogenous DA & NMDARs inhibitor - less glutamate)
Parkinson’s - DA R agonists
- Ropinirole (D2R agonist - non ergot)
2. Pramipexole (D3R agonist - non ergot)
Parkinson’s MAO-I, M1Rs & COMT inhibitor
- Selegiline (MAO-B inhibitor)
- Entecapone (COMT inhibitor - peripheral)
- Procyclidine & Benztropine (inhibit M1Rs - less tremor/dyskinesia)
Anticonvulsants - Grand mal txt
- Valproic acid (Inhibit Na chs, T-type Ca2+ chs, GABA transaminase, Increase K+ permeability in neurons)
- Phenytoin (Inhibit axonal Na+ chs - does not stop initiation of seizure. Non-linear kinetics)
- Carbamazepine (Inhibit Na+ chs, no inhibition of initiation
- Lamotrigine (AMPA-R glutamate antagonist & Inhibit Na+ chs - requires hepatic glucorunidation)
Anticonvulsants - Petit mal
- Ethosuximide (Inhibit T-type Ca2+ chs in thalamus)
- Clonazepam (BZD - long acting)
- Valproic acid
Anticonvulsants - Myoclonic seizures
- Clonazepam
- Lamotrigine
- Valproic acid
Status epilepticus treatment
- Bolus IV lorazepam/ midazolam/ diazepam
2. IV continuous for 5-20’ : Phenytoin/ Levetiracetam
Anticonvulsants - miscalleneous
- Vigabitrin (Inhibit GABA transaminase - partial & grand mal)
- Levetiracetam (SV2AR Block - no glutamate release. Broad spectrum)
- Phenobarbital (Barbiturate. GABA-A R allosteric binding)
Antipsychotics - 1st generation
Phenothiazines: Chlorpromazine (D2R, MRs, alphaR, H1R)
Butyrphenones: Haloperidol (D2R, MR, alphaR) & Droperidol (D2R, H1R)
Thioxanthene: Flupentixol (D2R, 5-HT, alphaR)
Antipsychotics - 2nd Generation Atypical (5HT2A Blockade)
- Clozapine (MAIN: D2R blocker. MR, alphaR, 5HT R block)
- Olanzapine (5HT, D2R block)
- Risperidone (5HT R block. No MR block)
- Aripirazole (PARTIAL D2R & 5HTR agonist)
- Tiapride (D2/D3 R antagonist)
- Cariprazine (D2/D3R antagonist - hungarian drug)
Bipolar Disorder treatment
- Lithium (Inhibit Inositol Monophosphatase - Decrease Gq, less Gs action)
Can add Carbamazepine & Valproate
Lithium Side Effects
- Flu-like symptoms
- GI distress
- Hypothyroid
- Nephrogenic DI
- Acute toxicity
- Teratogen - Ebstein’s anomaly
Tricyclic Antidepressants + Tetracyclic and Heterocyclic
- Clomipramine (TCA - Inhibit NET&SERT)
- Amitriptyline (TCA - Inhibit NET&SERT)
- Maprotiline (TetraCA - Inhibit NET more)
- Bupropion (HeteroCA - Inhibit DAT)
Serotonin Antagonist Antidepressants
Trazodone (Post synaptic 5-HT2A Receptor antagonist & SERT)
MAO Inhibitors
- Moclobemide (MAO-A - Antidepressant. Also inhibit Tyramine metabolism. Reversible)
- Selegiline (MAO-B - Parkinson treatment)
SSRIs
- Inhibit presynaptic reuptake of 5-HT*
1. Fluocetine (long T1/2)
2. Citalopram 1x20mg
3. Sertaline
1st line of treatment for depression & anxiety
SNRIs
- Inhibit NET & SERT. No cholinergic/adrenergic effect*
1. Venlafaxine (Panic, OCD, PTSD)
2. Duloxetine (Diabetic neuropathy)
3. Reboxetine (Selective NET)
Atypical antidepressants
- Mirtazipine (alpha2R selective antagonist - Increase presynaptic release of NE& 5-HT)
- Agomelatine (MT1R agonist & 5HT2&3R inhibitor)
- Tianeptine (GABA-R modulator, D2/3 R agonist, 5HT-R inhibitor)
Benzodiazepines
*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)
Non-BZD hypnotics
- Zaleplon (GABAa-R binding)
- Zolpidem (GABAa-R binding)
- Melatonin (MT1&MT2 Rs at suprachiasmatic nucleus of hypothalamus) - Sleep ONSET
- Ramelteon (MT1&MT2 Rs) - sleep ONSET
Non-BZD anxiolytics
- Buspirone (5-HT1 partial agonist)
2. SSRIs
Barbiturates
- Bind GABAaRs*
1. Thiopental - Short acting, induction of IV anesthesia
2. Phenobarbital - Long acting, Anticonvulsive (oral/IV)
IV anesthetics for induction
- Thiopental
- Propofol
- Etomidate (Bind GABAaR)
- Fentanyl
- Dexmedetomidine (cental alpha2 agonist - for ICU patients)
IV Anesthetics for maintenance
- Propofol (Potentiate Chloride current via binding GABAaR)
2. Fentanyl (opioid μ agonist)
Dissociative Anesthesia IV anesthetic
Ketamine (Inhibit NMDA-R complex)
CV stimulation
Conscious sedation IV anesthetic
Midazolam (antidote: Flumazenil)
IV anesthetics causing CV & respiratory depression
Thiopental, Propofol, Midazolam, Fentanyl
Inhaled anesthetics (Gas)
N2O
>100% MAC value
Inhaled anesthetics (volatile liquids)
- Desflurane (MAC: 6.5%)
- Isoflurane (1.4%)
- Sevoflurane (2%)
NOTE: Skeletal m. hypersensitivity => Malignant hyperthermia. Give Dantrolene
Narrow spectum, beta lactamase SENSITIVE
- Penicillin G (IV)
- Penicillin V (oral)
- Benzathine Penicillin G (IM depot shot)
Narrow spectrum, beta lactamase RESISTANT
- Nafcillin (IV)
- Oxacillin
* Do not cover MRSA*
Broad spectrum, beta lactamase SENSITIVE
- Ampicillin (IV)
2. Amoxicillin (pos) 3×500-1000mg
Extended spectrum, beta lactamase SENSITIVE
Piperacillin (IV)
Beta lactam combos
- Amoxicillin/ Clavulanic acid
- Ampicillin/Sulbactam
- Piperacillin/Tazobactam
Cephalosporins 1st gen
- Cefazolin (surgical prophylaxis)
- Cephalexin
Gram + cocci
Cephalosporins 2nd gen
- Cefoxitin
- Cefuroxime
Gram + cocci with gram - coverage
Cephalosporins 3rd gen
- Ceftriaxone (hospital acquired pneumonia & single IM dose for gonorrhea)
- Cefotaxime
- Cefixime
- Ceftazidime (pseudomonas)
Gram - increased coverage
Cephalosporins 4th gen
Cefepime (broad spectrum, beta lactamase resistant)
Pseudomonas!
Cephalosporins 5th gen
- Ceftaroline fosamil
- Ceftalozane/tazobactam
TREAT MRSA!
Probenecid inhibits tubular secretion of _____
- Cephalosporins
- Penicillin
- Methotrexate
Monobactam
Aztreonam
MOA: Bind PBP-3 ONLY in Gram- bacteria
(Klebsiella, Pseudo, Serratia)
Carbapenems (2nd gen)
- Imipenem (decrease seizure threshold)
- Meropenem
*Reserve Antibiotics, Pseudomonas. Resistant to most beta lactamases
Glycopeptide Antibiotics
MOA: Bind D-Ala-D-Ala, inhibit transglycosylation. BACTERICIDAL. Parenteral
- Vancomycin
- Teicoplanin
- Ortivancin
Lipopeptide antibiotics
MOA: Irreversibly inserts into cytoplasmic membrane, disrupt gradient. BACTERICIDAL
Daptomycin (MRSA, VRSA, VRE)
NOTE: causes rhabdomyolysis, be careful if patient takes statins too
Polypeptide Antibiotics
MOA: Inhibit peptidoglycan precursos translocation. Bactericidal/ Bacteriostatic
Bacitracin (topical due to severe nephrotoxicity)
Tetracyclines
MOA: Bind 30S. Bacteriostatic. Chelators (Ca, Fe, Mg). Accumulate in teeth - teratogen
- Tetracycline (pos)
- Doxycycline: first day 200 mg, than 100 mg 1x daily
- Tigecycline (IV only) - Glycylcycline
Aminoglycosides
MOA: Bind 30S, Needs O2 to penetrate cell wall (combine with beta lactams). Inhibit initiation complex, induces misreading of mRNA & inhibit translocation => Bactericidal
- Gentamycin - Tobramycin -Amikacin -Netilmicin
- Streptomycin (combine with penicillin)
- Neomycin - Kanamycin (Topical. Orally- remains active in GI tract)
Chloramphenicol
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
Oxazolidones
Linezolid
MOA: Bind 50S. Inhibit initiation complex for translation. Bacteriostatic
Inhibit MAO-A & B
MRSA, PRSP, VRE
Macrolides
MOA: Bind 50S. Bacteriostatic
- Erythromycin (txt walking pneumonia). Inhibit CYP450
- Roxithomycin (no activity against MRSA & PRSP). Inhibit CYP450
- Azithromycin 1x500mg for 3 days
- Clarithromycin. CYP450 Inhibitor
Ketolides
MOA: Similar to macrolides, especially erithromycin
Telithromycin (use for macrolide-resistant strains. CYP450 Inhibitor)
Clindamycin
MOA: Bind 50S. Bacteriostatic
Narrow spectrum. For Gram+ due to poor penetration of Gram - outer membrane.
NOTE: Can have C.difficile superinfection!
Streptogramin
MOA: Bind 50S - block exit channel on ribosome. Bactericidal
- Quinupristin
- Dalfopristin
Reserve antibiotics. CYP450 Inhibitor
Antimetabolite (antifolate) antibiotics
- Sulfonamides (Inhibit DHP synthase)
- Trimethoprim (DHF reductase inhibitor)
- Pyrimethamine/Sulfadiazine (Txt for toxoplasmosis)
- Proguanil (malaria prophylaxis)
TMP-SMX combo is bactericidal
Fluoroquinolones (-floxacin)
MOA: Inhibit DNA gyrase (topoisomerase II) in Gram - and Topoisomerase IV in Gram+
Bactericidal. Post Antibiotic effect
- Norfloxacin/ Ciprofloxacin/ Ofloxacin (2nd gen)
- Levofloxacin (3rd gen) - Respiratory walking pneumonia
- Moxifloxacin (4th gen)
Metronidazole
MOA: Forms free radicals
Bacteridical. High CSF concentration
CYP450 Inhibitor
Also used to treat protozoal diseases
Fidaxomicin
MOA: Inhibit bacterial RNA pol. Oral
Bacteridical
Can txt C.difficile
Rifaximin
MOA: Inhibit DNA-dep RNA pol
Rifampicin derivative
Use in Hepatic encephalopathy
Mupirocin
MOA: Inhibit bacterial protein synthesis by binding isoleucyl tRNA synthetase
Topical (not absorbed)
Fusidic acid
MOA: Inhibit bacterial elongation factor G
Bacteriostatic
Topical for skin infections & Oral for MRSA
Polymyxin E
MOA: cationic detergent. Bactericidal
Fosfomycin
MOA: Inhibit enolpyruvate transferase -> No N-acetylglucosamine (cell wall precursor)
Bactericidal
Nitrofurantoin
Urinary antiseptic
No systemic antibacterial effects
TB 1st line treatment
- Isoniazid (inhibit mycolic acid synthesis-Bactericidal -CYP450 Inhibitor)
- Rifampin (Inhibit DNA-dep. RNA pol - Bactericidal)
- Ethambutol (cell-wall synthesis inhibitor)
- Pyrazinamide (no known MOA. bacteriostatic)
RIPE - Phase I: 2 months
Phase II: 4-7 mo. Rifampin & Isoniazid
TB 2nd line
- Streptomycin/ Amikacin/ Kanamycin
2. Cycloserine (inhibit peptidoglycan synthesis)
Leprosy treatment
- Dapsone ( Inhibit folic acid synthesis - Bacteriostatic)
2. Rifampin
Antiherpetic agents
- Acyclovir (Inhibit viral DNA pol - HSV1/2, VZV & IV for HSV encephalitis)
- Valaciclovir/Famciclovir (Inhibit viral DNA pol - VZV & acyclovir resistant strains)
- Ganciclovir (Inhibit viral DNA pol - 1st line for CMV)
- Valganciclovir (ganciclovir prodrug with better oral bioavailability)
- Cidofovir (Inhibit Viral DNA pol - HSV, CMV, HPV, Adenovirus & TK- strains. IV)
- Foscarnet (not an antimetabolite - Inhibit both RNA&DNA pol - CMV 2nd line agent. IV)
Antiretrovirals - NRTIs
MOA: Prodrugs. Inhibit binding of nucleosides to reverse transcriptase
- Zidovudine - Pregnancy safe
- Lamivudine - also used for Hep B
- Emtricitabine - CI in pregnancy/child/ renal&hepatic Failure
- Abacavir
- Tenofovir - also used for Hep B. No phosphorylation needed for activation
- Stavudine (do not use with zidovudine)
- Didanosine - dose dependent pancreatitis
- Zalcitabine
Antiretrovirals - NNRTIs
MOA: Bind on reverser transcriptase (diff site from NRTIs). No phosphorylation needed.
Not active against HIV-2
- Etravirine (Inhibitor + Inducer of CYP450)
- Nevirapine (CYP450 Inducer) - Used to prevent vertical transmission
- Efavirenz (TERATOGENIC)
- Delavirdine (Teratogenic)
Antiretrovirals - Protease Inhibitors, Integrase inhibitors & entry inhibitors
- Maraviroc (Blocks CCR5 receptor so no interaction b/w viral gp120 and CD4 on lymphocytes)
- Elvitegravir (Bind integrase so viral DNA cannot integrate in host DNA)
- Ritonavir (PI - most common. MOST POTENT CYP450 INHIBITOR)
- Lopinavir (PI - use with ritonavir)
NOTE: Ritonavir is often added to HIV txt to increase serum levels of other antivirals due to CYP450 inhibition
Anti-influenza
- Amantadine/ Rimantidine (Inhibit M2 protein needed for onset of infection)
- Oseltamivir/ Zanamivir (inhibit neuramidase - no new virion clumping)
Anti-RSV
- Palivizumab (Human monoclonal Ab - no fusion)
2. Ribavirin
Hepatitis antivirals (non specific)
- IFN-α (activate cytokines, increase JAK-STAT path)
- Entecavir (guanosine analogue - Inhibit HBV DNA pol)
- Tenofovir (NRTI)
- Ribavirin ( Guanosine analogue, Inhibit IMP DH so no GMP. No Viral RNA pol)
Uses of IFN-α
Hep B, HHV-8, Hairy cell leukemia, malignant melanoma, papillomatosis, RCC, HPV
Hepatitis antivirals (DAAs)
- Paritaprevir/ Grazoprevir (PI - NS3/4A)
- Sofosbuvir (NPI - NS5B)
- Dasabuvir (NNPI - NS5B)
- Velpatasvir/ Elbasvir (NS5A)
Malaria drugs
- Chloroquine (Inhibit heme polymerization) + Hydroxychloroquine (less toxic and for AI)
- Mefloquine (Unknown MOA - blood schizontocide)
- Quinine (Inhibit protozoal DNA replication - schizontocide)
- Artemether (Produce free radicals - schizontocide)
- Lumefantrine (Unknown MOA)
- Malarone= Proguanil (Inhibit DHFR Thimydylate synthase) + Atovaquone (disrupt mitochondrial metabolism)
- Primaquine (Tissue schizonticide - oxidants)
Helminthic infections
- Mebendazole (Inhibit MT synthesis & glucose uptake)
- Ivermectin (Facilitate GABA-med. transmission thus immobilized parasites due to hyperpolarization)
- Niclosamide (Uncouple oxidative phosphorylation)
Antifungal agents
- Amphotericin B (Form pores in fungal membrane by interacting w/ ergosterol. Fungicidal)
- Nystatin (same as amphotericin but only TOPICAL due to toxicity)
- Clotrimazole (Imidazole. Topical, OTC. Interfere with ergosterol synthesis. CYP450 Inhibitor)
- Fluconazole (1st gen Triazole. Cross BBB so can txt Cryptococcus meningitidis. Interfere w/ ergosterol synthesis. CYP450 Inhibitor)
- Itraconazole ( 1st gen Triazole. CYP450 Inhibitor)
- Voriconazole (2nd gen Triazole, for Aspergillus. Cause Visual disturbances. CYP450 Inhibitor.)
- Flucytosine (5-FU, Incorporate into fungal RNA & Inhibit thimidylate synthase. Antimetabolite)
- Caspofungin (Echinocandin. Inhibit synthesis of beta(1,3) glucan of fungal cell wall
- Terbinafine (Inhibit squalene epoxidase - fungal membrane)
Disinfectants & Antiseptics
Alcohols: Ethanol 70%, Isopropyl alcohol 70-90%
Halogens: Povidone-iodine
Oxidizing agents: H202
Chlorinated phenols: Chlorhexidine
Cationic surfactant: Octenidin, Invert soaps