MBBS 1A & 1B PHARMACOLOGY

NMJ BLOCKING AGENTS MUSCLE RELAXANTS Class Drugs d-Tubocurarine Competitive (Non-Depol Agents) Pancuronium Gallamine Mivacurium Atcurium Vecuronium Description curare Potent (5x) Stabilizer Short Acting Intermediate Gen Anaesthesia Compete with Ach binding receptor Can be reversed by Ache inhibitors (i.e. Neostigmine) Muscle Relaxant (Surgery) Facilitate Intubation Orthopaedics (dislocate,#) Prevent trauma Diagnostic (MG) Histamine release Ganglionic blockade Tachycardia Hypertension MoA Uses Adverse P.kinetics 5-20mg: flaccid paralysis 10-20mg: apnoea

Toxicity: Oxygen AChE - Neostigmine Toxicity: Artificial Respiration Fresh Blood Transfusion +Halothane: hyperthermia (treat with Dantrolene)

Non-Competitive (Depolarizing Agents)

Succinylcholine

Fast! Short Duration

Phase 1: Depolarizing Phase 2: Desensitization Not Reversed by AChE

Facilitate Intubation

Bradycardia HypoKalemia Hypotension Post-Op SkM Pain Prolonged Apnea Hyperthermia Liver toxicity Eyelid Twitch (BS) Strabismus Dystonia

Dantrolene Direct Acting NM Relaxant

Inhibit Ca release

Malignant Hyperthermia

Botox

Blok Ach release in NMJ

Cosmetic

NON-STEROIDAL ANTI-INFLAMMATORY DRUGS Class Drugs Aspirin Ibuprofen Naproxen Diclofenac Indomethacin Piroxicam Ketorolac Paracetamol
(poor anti-inf action)

Description GIT CVS Hypothalamus Platlet Renal Uterus

MoA PGE2 + PGI2 + peptic ulcer PGF2 BE : Anti-Inflammatory PGE2 BE : Anti-pyretic (Fever) TXA2 BE : prevent clotting PGI2, PGE2 AE : Renal Flow PGE2 AE : Delayed Labour BE : Treat Senggugut

Uses

Adverse

P.kinetics Contraindicate: PUD Bleeding Pregnancy Breast feed CHF Renal Disease Leukotrienes : Bronchoconstriction Rashes, Angioedema

Pain (Headache, Myalgia etc.) Fever Osteoarthritis Prevent Clotting Post-MI (aspirin) In MoA

(Non-Selective COXi) tNSAIDs

Preferential COX-2i

Nimesulide Meloxicam Nabumetone Celecoxib Itoricoxib Parecoxib ANTI-ARRYTHMIC

Not-Significant

Selective COX-2i

Arthritis Dysmenorrhoea Familial Ad Polyposis

COX-1 +TXA2: Non-Cardioprotective CI : CHF, HTN

Class

Drugs Disopyramide

Description

MoA Block Na channel (moderate) Block K channel

Uses Life threatening V-arryth

Adverse

P.kinetics Moderate Phase 0 Depression Prolonged Repolarization Duration of AP Weak Phase 0 Depression Shortened Depolarization Duration of AP Strong Phase 0 depression No effect of depolarization No change on AP Stabilize HR

Class Ia

Quinidine Procainamide Lidocaine

DOC

A/V arrhythmia

Class Ib Phenytoin Flecainide Class Ic Propafenone Class II Esmolol Atenolol Amiodarone Class III Sotalol Class IV Verapamil BB

Block Na channel (weak)

Digitalis-Associated Arrythmia SV arrhythmia V arrhythmia Exercise-Induced Arryth.

Block Na channel (strong) Block Ca channel (weak) Block E, NE Receptor

Block K channel

SV arrhythmia V arrhythmia AV Conduction in A.Fib

Delayed in Repolarization Prolonged Ref. Period AP Duration

Block Ca channel Block Na Channel ( Intracell Na) Increase Cytosolic Ca Increase Contraction Vagus (+sympathetic)

Non-Classified

Digoxin Atropine Adenosine Mg2SO4 First-Line

Atrial Fibrillation Bradycardia / Heart Block SV arrhythmia Torsades-de-Pointes Quinidine-Induced Arryth

LIPID LOWERING Class HMG-CoA reductase Inhibitor (statins) Drugs Atorvastatin Long Acting Rosuastatin Simvastatin Gemfibrosil Fibrates Fenofibrate Bezafibrate FFA Liver formation of Hepatic VLDL circulating TG Fibrates + PPRA LL VLDL (TG) Hyper TG Short Acting HMG-CoA HMG-CoAr Description MoA Uses Hyper LDL Adverse Headache GI upset Muscle tender (CPK) Myalgia Hepatitis Gall Stones Skin Flush, Heat Dyspepsia, Vomitting Liver Toxicity Reversible Liver Impaired HDL P.kinetics

Cholestrol

Atheroma rupture LDL-Oxidation Endothelial function

Take at bedtime (HMG-CoAr )

G + Statin = myopathy F/B + Statins = Safe

Nicotinic Acid

Niacin

+ HDL

Hyper TG

+ Statins = myopathy

Ezetimibe Drugs Statins Fibrates Niacin Ezetimibe

Inhibit cholesterol absorption LDL ANTI-ANGINAL

Hyper LDL TGL

Combine with statins

Class

Drugs Nitroglycerin

Description Sublingual

MoA Venodilate (Preload) Artery Dilate (Afterload)

Uses Unstable Angina CHF Acute LVF Acute MI Cardiac Procedures DVD: Angina, HTN VD: SV arrhythmia V: migraine prophylaxis

Adverse Headache Reflex Tachycardia Postural Hypotension Constipation Peripheral Edema Hypotension Reflex Tachycardia (Worsen Angina)

P.kinetics + sidenafil - BP Less FPM

Organic Nitrate

Isosorbide-Dinitrate Isosorbide-5-mono Nifedipine DHP (VD) VD, FC, HR VD, FC, HR

CCB

Amlodipine Verapamil Diltiazem

HR, FC O2 demand Artery Dilate TPR / afterload Coronary flow

Reflex Tachycardia: Amlodipine DHP + Beta-Blocker

Atenolol Beta-Blocker Metoprolol Propanolol Timolol Late Na Current Block Ranolazine Low-Dose Aspirin Anti-thrombotic Heparin Warfarin

B1-Selective HR, FC O2 demand B1 + B2 Ca in Myocardium

Prophylaxis: Myocardial Infarction Angina Angina Torsades de Pointes

(more important in CHF)

No effect on HR, BP

Prevent clotting ANTI-HYPERTENSIVE

Angina

Bleeding

Combination Therapy

Class

Drugs Pra^zosin Tera^zosin

Description

MoA

Uses Hypertension BPH

Adverse Ortho. Hypotension Reflex Tachycardia Nausea Rhinitis Urination Tiredness Depression Dry Mouth

P.kinetics

Selective

Block 1 VD (BP)

1-blocker

Doxa^zosin Phenoxybenzamine Phentolamine Clonidine Non-selective Irreversible Central Acting + Imidazoline B1 Selective B1 + B2 B1 + VD B1 + B2 + VD B1 + B2 + 1 Na/Cl Na Blocker X-Aldosterone Volume BP Hypertension Edema 1. HR, FC CO 2. X-B1 X-Renin X-AT2 3. Block 1 VD 4. Nebivolo +NO Hypertension Angina Post-MI CHF Block 1 + 2 Pheochromocytoma

2-agonist

Methyl Dopa Menoxidine Atenolol Timolol

sympathetic activity (E, NE) VD Artery

Hypertension Menopause

CI: Renal Failure

Beta-Blocker

Propanolol Nebivolol Pindolol (ISA) Carvedilol Thiazides Amiloride

Asthma (B2) ++ COPD Bradycardia Tiredness

CI: Asthma (B2) ISA (Intrinsic Sympathomimetic Activity)

Hypokalemia CI: Hyperuricaemia

Diuretics

Triamterene Spironolactone

Hyperkalemia

Alis^kiren Val^sartan RAAS Irbe^sartan Telmi^sartan Enala^pril CCB VD Hydralazine Na Nitroprusside Class Drugs

Renin Inhibitors Hypotension Headache Angioedema

ARB

*Refer RAAS

Hypertension

ACE Inhibitors DHP + Diltiazem Artery Dilator Nitro VD Congestive Heart Failure (CHF) Description MoA Uses CHF: Class 2, 3, 4 (+ symptoms) Adverse P.kinetics Diuretic Resistance: Excess Na Intake +NSAIDs Renal Impaired VD BP Hypertension Myocardial Ischemia Peripheral Edam Hyptension Reflex Tachycardia

Frusemide

Diuretics

(X-Na-K-Cl) : Preload

Hypomagnesemia

Preload

Enalapril Ramipril Lisinopril Nitroglycerin Venodilators Artery Dilator VD Preload Limit Ca Relax Smooth Muscle CHF: 2,3 + HPT Beta-Blockers HR Cardiac Remodelling O2 demand CHF + A.Fib CHF ACE Inhibitors X-AT2: VD, Aldosterone Hypertension

Hypotension Headache Dizziness Hypotension Sublingual / IV + sympathetic reflex (CI: angina + MI) Asthma (B2) Bradycardia Paraesthesia Notes Toxicity AV Block Sinus Bradycardia SV Arrhythmia V Arrhythmia Treatment Atropine Atropine Propanolol Lignocaine

Afterload

Hydralazine Metoprolol

Oxidative Stress

Atenolol Carvedilol

Worsen CHF (HR)

Contractility

Digitoxin Class I

Glycosides No Symptoms S + Mid Exertion S + Less Exertion S at Rest

X-Na/K: FC SV Peak Tension + Velocity (Systole shorten Diastole prolong) ACEI + BB ACEI + D + BB + G ACEI + D + BB + G + VD All + IV D + IV VD + IV G

Notes:

Class II Class III Class IV

BRONCHIAL ASTHMA Class B2 Agonist Leukotriene Inhibitor Anti-cholinergic Adrenergic Agonist Drugs Salbutamol Theophylline Ipratropium Br Epinephrine (E) Budesonide Beclomethasone Formoterol Salmeterol Zafirlukast Montelukast Cromolyn Sodium Drugs Lozenges Demulcents Syrups Potassium Iodide Expectorants Guafenesin Mucolytics Bromhexine Codeine Opioid Antitussives
(suppress or relief cough)

Description Selective SABA

MoA ACUTE TREATMENT +B2 : Bronchodilate X-Leukotrienes: Bronchoconstrict - Muscarinic : Bronchodilate cAMP : Bronchodilate PROPHYLAXIS

Uses First-line Asthma Asthma, COPD Second-line Asthma Asthma, Allergy

Adverse Tremor + Anxiety Arrhythmia, CNS + Sedation, Dry Mouth Tachycardia

P.kinetics MDI (Inhale) Found in Coco MDI, Nebulizer Oral

Glucocorticoid B2 Agonist Leukotriene Inhibitor Mast Cell Stabilizer Class

AntiInflammatory Selective LABA

Suppress Immune : X mucus +B2 : Bronchodilate X-Leukotrienes: Bronchoconstrict X Histamine Release COUGH

Chronic Asthma Nocturnal Asthma Exercise-Induce Asthma Allergic Uses Symptomatic Relief

Super infection Wheezing Eosinophilia, Rash Dry Mouth Adverse

Oral, Parenteral >12h + Glucocorticoids Oral, Children MDI, DPI + LABA P.kinetics Short Acting Effects Vanish w Layer

AntiInflammatory

Description

MoA +salivation +viscid layer sooth

SSKI

Secretion Secretion + Ciliary Action Secretion + Ciliary Action

Productive Cough Asthma Productive Cough

Gastric Irritant Nausea Tears + Runny Nose Constipation Respiratory Distress

Require hydration
SSKI: Saturated Solution K Iodide

Add in syrups

Suppress cough center selectively

Unproductive cough

Add with NSAIDs

Pholcodine Noscapine Non-Opiod Dextropethorphan Activate sigma receptor Unproductive cough

Nausea + Vomitting

Diphenyhydramine Promethazine Anti-Histamine Cetrizine (Zyrtec) Loratidine (Claritin) Levocetirizine Fexofenadine Decongestants Ephderine Pseudoephderine Drugs Ferrous Sulphate Ferrous Fumarate IRON Ferrous Gluconate Iron Dextran Iron Sucrose Cyanocobalamin B12 Hydroxycobalamin Folate

1 Generation 2 Generation 3 Generation Sympathomimetic

rd nd

st

Block H1 receptor Block H1 receptor Block H1 receptor +Adrenergic VC Blood HEMATINIC : + RBC

Allergic rhinitis Allergic rhinitis Allergic rhinitis Nose blocked

Dizziness, Drowsy Dry mouth Blurred Vision Safer Insomnia, Anxiety

Cross BBB Not cross BBB Non drowsy Rapid Action CI: Hypertension

Class

Description Dissociable Ferrous Salt

MoA

Uses Iron Def. Anemia

Adverse Epigastric pain Nausea Metallic Taste GI Upset

P.kinetics Empty Stomach

*not significant Parenteral Iron Def. Anemia Pernicious Anemia Tapeworm Ileectomy Megaloblastic Anemia Pregnancy (NTDs) Renal Failure Chemotherapy

CI: Pregnant, Infants, Children, GIT Bleed CI: Folate Def. Anemia

+ Intrinsic Factor Absorbed PP Bound Increase folate

Allergic

Allergic Blood Viscosity + Clot Flu-Like Symptoms

CI: Pernicious Anemia

EPO

Epoetin Alpha

Recombinant

+ BM to produce RBC IMMUNOSUPPRESSANT

IV

Class

Drugs Azathioprine Cyclophosphomide Mycophenolate mofetil

Description Non-Selective

MoA + 6-mercaptopurine (Purine Analogue) IMP X Guanylyl (de novo) T-cell Activation

Uses Inf. Bowel Disease Rheumatoid Arthritis Prevent Graft Rejection Lymphoma

Adverse BM Suppression Liver Impair GI ulceration, Edema Hypertension, Edema

P.kinetics CI: Allupurinol

Anti-proliferative

mTOR Inhibitor

Sirolimus

CI: Lung Transplant

Cyclosporine Calcineurin Inhibitor Tacrolimus Prednisone Corticosteroids Dexamethasone Basiliximab IL-2R Inhibitor Daclizumab Steroid

Bind to Cyclophilin X-NFAT : IL2 - T-cell Division

Graft Rejection

Hypertension

CI: Renal Impaired

Supress IL2

Allergic, Autoimmune

Weight Gain, Anxiety

Slow Withdrawal

Block IL2 Receptor

Prevent Graft Rejection

Opp. Infection

ANTICOAGULANTS & THROMBOLYTICS Class Drugs Streptokinase Fibrinolytic Urokinase Alteplase Heparin Enoxapain LMW Heparin Tinzaparin Anticoagulant DVT Pulmonary Embolism Unstable Angina + MI High PP Bound Start w Heparin (5 Days) Antidote: Vit K Unstable Angina Less Description Antigenic Non-Antigenic Human tPA Bleeding, Osteoporosis Monitor aPTT Stroke Acute MI ++ Pulmonary Embolism Systemic Lytic Hemorrhage MoA Uses Adverse P.kinetics

X-F10a Selectively Thrombocytopenia

Warfarin

Oral

Bleeding Teratogenic

LD Aspirin Anti-Platlet Drugs Clapidogrel

75 135 mg

LD: X-TXA2 HD: X-PGI2

ADPr Inhibitor Abciximab

Bind to GP IIb/IIIa

Prophylaxis: MI, Angina Transient Ischemic Attack Stroke Coronary Angiplasty Peri. Vascular Disease

GI Bleed GI Irritation Allergy Thrombocytopenia

PEPTIC DISEASE Class Drugs Cimetidine H2-R Blocker Ranitidine Famotidine Nizatidine Omeprazole PPI Lansoprazole Pantoprazole Rabeprazole Oral IV Duodenal Ulcer Gastric Ulcer GERD, ZE Syndrome NSAIDs Induce Ulcer Nausea Headache Abdominal Pain Muscle Pain Abdominal Cramp Diarrhoea Uterine Bleed + Enteric Coated (ionized at pH <5) Absorb in Canaliculi Description MoA Uses Duodenal Ulcer Gastric Ulcer GERD ZE Syndrome Adverse P.kinetics Enzyme Inhibitor Anti-Androgenic Good Oral Antacids Absorption

Headache Dizziness Bowel Upset

PG Analogue

Misoprostol

+PGE2, I2 : mucus secretion

Prevent NSAIDs Ulcer Induce Labour

4x/day dose

Na-Bicarbonate Na-Citrate Antacids Mg-Hydroxide Al-Hydroxide Mg-Trisilicate Sodium Alginate Ulcer Protective Sucralfate Omeprazole H. pylori Tinidazole Clarithromycin Amoxicillin Class Drugs Metoclopramide Domperidone

Systemic

pH of Stomach Gastritis Systemic Acidosis GERD Al: Osteoporosis Mg: CNS Depression

Non-Systemic MMT Gaviscon Sticky Gel PPI pH : Bacteriocidal Antiobiotics Coat Ulcer Base

Insoluble Take w Meals 2 3 hr Action CI: Fluoroquinolones

Peptic Ulcer Disease

q.i.d + 1hr before meal

Triple Drug Therapy

*Refer PPI

b.i.d 2 weeks

VOMITTING, DIARRHOEA & CONSTIPATION Description MoA Inhibit D2 Receptor: (CTZ) LES Tone Peristaltic Relax Pyloric Sphincter Uses Vomitting (X-labyrinth) GERD, Dyspepsia Emergency Surgery Adverse Cross BBB Dystonia Extra-Pyramidal Effects Not Cross BBB P.kinetics Toxicity: +Promethazine

D2 Blocker

Prokinetic

5-HT3 Blocker

Odan^setron Grani^setron Scopalamine Dicyclomine Prochlorperaqzine

Anti-Emetic

Block 5-HT3 Receptor (CTZ, GIT)

Vomitting (X-Labyrinth) Drug Induced Vomitting

Headache Constipation Dry Mouth Constipation Blurred Vision Sedation Psychomotor Control

5-HT3 = Serotonin Transdermal Patch + with Ototoxic Drugs (Aminoglycosides) + D2 Blocker Toxicity

M Blocker

Block M Receptor (CTZ, Labyrinth) Anti Motion Sickness Block H1 Receptor (CTZ, Labyrinth) CB1R Agonist Immunosupp. Description Diet Stool Softener *not significant GI MOTILITY Anti-Chemo Vomitting Prevent Motion Sickness Otitis

H1 Blocker Adjuvants

Promethazine Diphenyhydramine Dronabinol Corticosteroids Drugs Fibre Docusate Sodium Liquid Paraffin Bisacodyl Purgatives Na Picosulfate

Psycho Effect Sympathomimetic

Class

MoA Retain water Volume Stool Surface Tension Lubricates Hard Faeces Secretions + Peristaltic

Uses Functional Constipation Constipation Constipation Constipation

Adverse -

P.kinetics 2-3 days for effects

1-3 days Abdominal Cramp

Constipation Pre-Surgical Cleansing Saline Laxative Retain water in lumen Chronic Constipation 5-HT4 cAMP : Secretions IBS, Chr Constipation Pro-kinetic Rehydration + Bowel Distension : + Evacuation Replace Fluid + Electrolyte Diarrhoea Abdominal Cramp agonist : Activity Opiod X-Enkepalinase cAMP Non-Infective Diarrhoea Cross BBB Nausea CI: Children Chronic : IV Flatulence, Nausea Fructose + Lactose

Laxatives Mg Sulfate Lactulose Mosapride Tegaserod Enema ORS Loperamide Anti-Motility Diphenoxylate Racecadotril Flatulence Non-Compliance

DIABETES MELLITUS Class Drugs Glyburide Glipizide Gliclazide Glimepiride Insulin Secretagogues Repoglinide Meglitinide Nateglinide Block S-R K Ca Influx Metformin Insulin Sensitizers Pioglitazone Thiazolidinedione Rosiglitazone Acarbose Glucosidase Inhibitor Miglitol Inhibit DPP4 : Incretin Degrade insulin secretions Glucose Uptake Hepatic Glucose Production INSULIN Class Rapid Acting Aspart Short Intermediate Regular Isophane Lente 6 8 hours 20 24 hours Drugs Lispro 3 -5 hours Description MoA Uses PPBG Control ( Hypoglycaemia) Ketoacidosis (IV) Adverse P.kinetics Subcutaneous Dose = meal 5 15 min a/c 30 min a/c Suspension Lante X Regular HbA1c 0.7 1.3% Biguanide SKM: Glucose Uptake Liver: Gluconeogenesis Activate PPAR- SkM: Uptake, FA Flux, Insulin Resistance Liver: Gluconeogenesis HbA1c 1-2% Diarrhoea Nausea Abd Discomfort Anorexia Metal taste Metformin : DOC Take with Meals No Weight Gain CI: Renal Impaired HbA1c 1-2% Headache Joint Pain Weight Gain Take 10 min before meal ( PP Insulin +) Hypoglycemia Sulfonylurea Normalization of FBS, PPBG Liver Failure Renal Failure Take 30 min before meal ( Basal Insulin +) Description MoA Uses Adverse Hypoglycaemia Weight Gain P.kinetics : BB, NSAIDs : Steroids

Abdominal Discomfort Flatulence Bloating

Take with first bite

DPP-4 Inhibitor

Sitagliptin

HbA1c 0.7 0.8

Nasal Mucosa Inflamed + UTI

Incretin: GLP-1, G1P

Ultra-Lente Slow Determir Glargine

36 hours Ph 5.4 (Dont Mix) 14 hours 24 hours ANTI-THYROID Peakless : Night Use

Class

Drugs Propylthiouracil

Description

MoA Inhibit Thyroid Peroxidase: X: Iodide tyrosyl X: Iodide X: Coupling (MIT, DIT) X: Peri. Deiodination (T3 T4) Block Na/I Symporter ++ Iodide Thyroid Constipation

Uses

Adverse Maculopopular Rash\Arthralgia Agranulocytosis Hypothyroid Baby

P.kinetics Less potent : q.i.d Not Cross Placenta More Potent : b.i.d Cross Placenta *Obselete + Thioamide Agent CI : Pregnancy

Anti-Thyroid Methimazole Thiocynates Perchlorates I Radioactive Iodine I

127 131 123

Prep Surgery Control hypersecretion Definitive Treatment

Ionic Inhibitor Iodides

Clinically Not Used Prep Surgery I

123

Aplastic Anemia Metallic Taste Edema + Swelling I

131

Trapped in thyroid + with iodotyrosine Colloid Scan HR ADRENOCORTICOSTEROIDS

- Thyroid Scan

I Beta - Blocker

*not fir for surgery Control symptoms of hyperthyroidsm

hypothyroidism (follicular necrosis)

Propanolol Atenolol Drugs Description

Class

MoA Glucose: Gluconeogenesis, Uptake Lipid: Fat Redistribution: Buffalo Hump, Moon Face

Uses

Adverse

P.kinetics

Steroid

Corticosteroid

Glucocorticoid Mineralocorticoid

Fluid & Electrolyte: Aldosterone Skeletal Muscle: Weakness, Myopathy, Ca CNS: Mood, Psychosis Stomach: ++ peptic ulcer Anti-Inflammatory: Lipocortin

Addisons Disease Rheumatic Disease Renal Disorders Allergic Reaction Bronchial Asthma Infectious Disease Ocular Disease Skin Disease GIT Disease Chemotherapy

Skin: Delayed Healing MSSK: osteoporosis CNS: Psychoses Endocrine: Hypogonad CVS: Hypertension Immune: Opp. Infxn GIT: Peptic Ulcer

Most: Oral Dexamethasone: IM/IV Insoluble: Intradermal Local: Aerosol, Topical

KIDNEY Class Drugs Frusemide Loop Diuretic Torasemide Hydrochlorothiozde Thiazides Polythiazide Indapamine Chlorthalidone Spironolactone X-Aldosterone K+ Sparing Eplerone Amiloride Triamterene Osmotic Diuresis CA Inhibitors Dorzolamide Mannitol Acetazolamide X-ENaC Block Aldosterone Receptor Late Distal Tubule + C.Duct ( Na, H20 + K secretions) X-ENaC Collecting Duct ( Na, H20 Secretions) GFR (Prox. Conv Tubule) X-CA : X formation of H2CO3 (+ Metabolic Acidosis) Secretions of Na, K, Cl, HCO3 ORAL CONTRACEPTIVES Class Combined Drugs Oestrogen Progesterone Oestrogen Sequential Pill Mini Pill Post-Coital Implant Vaginal Hormone Transdermal O+P DF Progesterone Mifepristone Norgestrel Norplant Nuvaring Norgestimate 16 days 5 days 7 days Low Dose 72 hours 12 hours 6 Levonorgestrel EE + Etonogastrel EE + Norgestrmn Contraceptives Modify F. Tubes contraction Implantation of Blastocyst Gn Release X-FSH + LH Peak X Ovulation Oral Contraceptives Thrombophlebitis Thromboembolism Hypertension Cancer Gall Stones CI: Hypertension X-antibiotics X-Enzyme Inhibitors Less Effective + IUD after 5 days Most Effective Flexible (Upper Vagina) Description MoA Uses Adverse P.kinetics Hyperaldosterone (Conn) Hypertension, Edema Hypertension, Edema Cerebral Edema Glaucoma Altitude Sickness Allergic Bone Marrow Suppress X-Na/Cl Symp X-Na/Cl Distal Conv. Tubule (Block NaCl Reabsorption) X-Na/K/Cl Symp Description MoA X:Na/K/Cl Thick Asc. Limb (Block NaCl Reabsorption) Uses Pulmonary Edema Cardio + Renal Edema Forced Diuresis: Overdose Hypertension Cardio + Renal Edema Kidney Stones Adverse Fluid & Electrolyte Imb Alkalosis Ototoxicity Hypomagnesemia Fluid & Electrolyte Imb Uricaemia Sexual Dysfunction Photosensitivity Altered Sexual Character Hyperkalemia (K) Photosensitivity P.kinetics X-Sulfonylurea X-NSAIDs

X-NSAIDs () X-Digoxin () +K sparing (Amiloride)

CI: Hyperkalemia (K) *ENaC: Epi Na Channel + Thiazides ( K loss) CI: Edema Not useful to mobilize edema

Copper IUD Progesterone Levonorgestrel PARKINSON Class Drugs Description MoA Uses Adverse GI Upset Ortho. Hypotension CNS: confusion Similar to L-Dopa Retroperi. Fibrosis Digital Vasospasm Dry Mouth. Insomnia Drowsiness Confusion Dry Mouth Hepatotoxicity Lethargy, Insomnia Adverse Less Efficacious P.kinetics P.kinetics + Peri. DopaDecarboxylase Inhibitor (Carbidopa) +Drug Holiday Pergolide DA-R Agonist Bromocriptine MAO-I Selegiline Diphenyhydramine Muscarinic Antagonist Benztropine Bipiredin COMT-I Anti-Parkinsonism Class Tolcapone Entacapone Amantidine Drugs Triazolam Midazolam Lorazepam Benzodiazepines (TLAD) Quazepam Alprazolam Clonazepam Diazepam Flurazepam Adjuvant Anti-Viral Description Rapid-Acting (<6 hours) Short-Acting (10-12 hours) Intermediate (12-18 hours) Long Acting (12-24 hours) The amount of L-Dopa Cross BBB Alter uptake + release of DA SEDATIVES & HYPNOTICS MoA Uses Surgery Transient Insomnia Short-Lived Anxiety Tension induced psychosis Anxiety + Depression Acute Panic Attack Organic Disease CNS Depression Psychomotor Imp. Cognitive Imp. Ataxia Dependence Teratogenic Adjunct: L-Dopa/Carbi Mild PD ACh Block Ach Receptor Drug-Induced PD (metoclopromide) X-MAO-B Ergot Alkaloids +DA Receptor at Corpus Striatum (+ GP internal) Selective Irr. Inhibit MAO-B DA Breakdown, DA Effects Advance PD Start w Low Dose

DA Precursor

Levo-dopa

DA in Basal Ganglia

Parkinson

Early Mild PD

X-Cheese ( Tyrosine) Start w Low Dose CI: BPH, Glaucoma

CI: Pregnant Flunirazepam: Date-Rape Overdose : Flumazenil X- Enzyme Inhibitors (Cimetidine, MOA-I)

Enhance GABA Effects in CNS (+GABA-A Receptor)

Zolpidem Non-Benzodiazepines Atypical Anxiolytics Beta-Blocker Zaleplon Zopiclone Buspirone Propanolol Melatonin Misc. Promethazine Opiod Amytriptyline Class Drugs SSRIs, TCA OPIOD ANALGESICS Description MoA Analgesic Pathway - Sensory Limbic Tranquillity, Euphoria Locus Cerulus - Fear, Anxiety Cough Center - Cough Respiratory Center - Resp. + CTZ-Vomiting EWN-Pupil Constriction (Pin-Point) +Histamine : VD, Skin Itchy Pain - CO Cardio-protective GIT: Peristaltic, Secretions Spasm of Sphincter of Oddi Morphine Congeners Cough Center Uses Adverse Nausea, Vomiting Constipation Biliary Tract Pressure Urinary Retention Hypotension, Pruritus Drowsiness Mental Clouding Resp Depression Constipation Drowsiness Nausea, Vomiting Constipation + Dependence Resp. Depression Tachycardia (IV) Pupil Dilation + Dependence Hypoventilation P.kinetics + Tolerance + Dependence + Abuse Precaution: Pulmonary Disease Hypotension, Shock (VD) Head Injury (ICP by CO2 Retention) Neonate Renal, Liver Impaired Less Analgesic Effects Better Oral Efficacy Less Resp. Depression Less Constipation Aka: Meperidine,Demerol CI: MAO-I 100x Analgesic: Morphine Rapid + Short Acting Anti-Depressant Anti-histamine Serotonin 5HT1A Partial Agonist X-Beta Adrenergic Receptor GAD:Gen Anxiety Disorder Performance-Induced Reset Circadian, Jet Lag Surgical Prep Note: Sedative : + calm Hypnotics : + sleep Dizziness, Nausea Less Sedation & Depndce Bind to GABA-A Receptor Insomnia Hallucinations Amnesia CI: Driving, Elder, GERD

Morphine

Cancer Pain Fracture Pain Post-Op Pain Biliary Colic MI, LVF Balanced Anesthesia Visceral Pain (X-MSSK)

agonist

Codeine

Dry Cough, MSSK Pain Depression Fibromyalgia

Tramadol

Serotonin, NE Reuptake

Pethidine

Bind to , and also receptor

Obstetrics (Labor Pain) Epidural: Post-Op, Labor Transdermal: Cancer IV: During Surgery

Fentanyl

Bind to receptor

Methadone

Bind to receptor

Treat Heroin Addicts

Biliary Pressure Constipation Irr. Resp. Depression Hypotension Blood Pressure Hallucinations Tachycardia Dysphoria Dysphoria Sudden Chest Pain Nausea, Vomiting Anxitey + Sweating

Less Euphoria Long Duration CI: Labor Pain High Lipid Soluble (Sublingual) CI: CHF, Renal Impaired

Partial Agonist

Buprenorphine

Partially bind to receptor

Rehab, Cancer Pain Post-Op Pain

Agonist

Pentazocine

Activating receptors on Sp. Cord

Moderate to Severe Pain

Nalbuphine Naloxone antagonist Naltrexone Oral IV

Bind to receptors Bind with high affinity to opiod receptors ANTI-MALARIA

Chronic Pain Opiod Poisoning Neonatal Asphyxia Heroin Addicts Alcohol Abuse Uses

+ Ceiling Effects 0.4 mg every 2 mins Longer Duration

Class

Drugs

Description

MoA

Adverse GI Upset (Nausea + Vomitting) Visual Disturbance Cardiac Arrhythmia Irrv. Retinopathy

P.kinetics Very High Vd T1/2 = 1-2 months High Dose: Cardiotoxic

Chloroquine

DOC

Interfere w Parasite Heme Detox

Clinical Cure Radical Cure Chemoprophylaxis

Quinine Clinical Cure (Blood Schizont) Arte-meter (methyl ether) Arte-sunate (Hemisuc. Ester) Arte-ether (Ethyl Ether)

Cinchona Tree

Interfere w Parasite Heme Detox

Clinical Cure

Cinchonism Hypoglycaemia Renal Failure

More Cardiotoxic 95% PP Bound Lipid Soluble

X-Ca. Adenosine Triophosphatase Artemesinins ACT:

20mg Artemeter + 120mg Lumefantrine Artesunate + S/P Artesunate + Mefloquine Quinine + Doxycycline

Clinical Cure Infection Control (Gametocidal)

Allergic Mild GI Disturbance Dizziness Tinnitus Liver Enzyme ECG Abnormality

CI: First Trimester

Water Soluble

Gametocidal Primaquine Radical Cure Mefloquine PYR+Sulfadoxine Others Lumefantrine Doxycycline Proguanil Class Drugs Chemoprophy. ANTI-TUBERCULOSIS Description MoA Clinical Cure (+Artesunate) (+Artesunate) (+Artemether) (+Quinine) Unknown

Radical Cure Infection Control Prevent Relapse (Kill Hypnozoites)

Abdominal Pain GI Upset MetHbnemia + cyanosis ACT Rationale: Resistance to Chq Protect resistance declined efficacy More effective

CI: G6PD

P. falciparum: 20x merozoites Cerebral toxicty Bilirubin load Hypovolemia Chq Resistance

Uses Bactericide:Rapid Multiply Bacteristatic: Slow Grow Intra & Extracellular Bactericide: All Subpop. (Except DormanT) Intra & Extracellular Resistance Prevention

Adverse Hepatic Toxicity PNS & CNS Toxicity Urinary Retention + Resistance

P.kinetics Enzyme Inhibitor I: Phenytoin

Isoniazid

INH

Inhibit Mycolic Acid (Cell Wall)

X-DNA-Dependent RNA Polymerase Rifampicin X RNA Transcription

Hepatitis Flu-Like Syndrome Orange Body Secretion

Enzyme Inducer

Anti-Tuberculosis Pyrazinamide PZA

Pyrazinamidase convert PZA to Pyrazinoic Acid (active form) ++ Disrupt Membrane Potential Interfere with Energy +

Short-Term therapy for Uncomplicated TB Intracellular Decrease Relapse Rate

Liver Damage Hyperuricemia + Gout Arthralgia Rash + Fever

Bacteriostatic

Ethambutol

EMB

Inhibit Cell Wall Synthesis

Combination Therapy Suppress Growth Res. TB

Visual Disturbance

CI: Children (< 6 y/o)

Streptomycin

Aminoglycoside

Bind to 30S Interfere Proofread

Extracellular

X-Vestibulocochlear (8) Nephrotoxicity

IM Injection only

ANTIBIOTICS Class Drugs Description MoA Uses Drug of choice: M. pneumonia Chlamydia Diphteria Pertussis H pylori H influenzae Salmonella Toxoplasmosis Alternative: Tetanus Strep Tonsillitis Pharyngitis Pneumonia Prophylaxis: Rheumatic Fever Endocarditis Adverse Skin Rash Thrombophlebitis GI Disturbance Torsades-de-Pointes Skin Rash Nausea + Vomitting Jaundice AAD Abdominal Pain Nausea + Diarrhoea Cholestatic Hepatitis AAD P.kinetics X-Cross BBB Phagocytosis into Synovial Eliminated in Bile Enzyme Inhibitors ( AE of other drugs) X-statins: Rhabdomyolysis + myopathy X-OCS: Loss Effectiveness H pylori (Clarithro + Amoxicillin)

Erythromycin

Gram +ve Resp. Tract Infxn

Bind to 50s Macrolides Clarithromycin X-Translocation

Gram ve H. influenzae H pylori Pharyngitis Resp. Tract Infxn Gonorrhoea

PROTEIN SYNTHESIS INHIBITORS

Azithromycin

Thyphoid Chlamydia T gondii Bind to 50s X-Translocation Bind to 50s X-Translocation 3 7 Narrow-Spectrum 1 Generation 2 Generation 3 Generation 4 Generation
th rd nd st

Ketolides

Telithromycin Clindamycin Lincomycin Quinupristin

S. pneumonia (Erythromycin Res) H influenzae, B pertussis Gram +ve (MRSA), Anaerobic Protozoa (Malaria)

*same as Clarithro Thrombocytopenia Diarrhoea, Rash Nausea Myalgia + Arthralgia Teratogenic Jaundice Nausea + Vomiting Allergic CNS Effects Arthropathy

10x affinity for 50s bind than erythromycin Topical: Acne Treatment

Lincosamides

Streptogramins Dalfopristin Fusidic Acids Sodium Fusidate Norfloxacin Fluoroquinolones Ciprofloxacin Levofloxacin Trovafloxacin

Bind to 50s Dalfopristin change ribosome structure + Quinupristin bind Bind to 50s X-Translocation X-bDNA gyrase X-Supercoiling X-bDNA synthesis

Gram +ve : MRSA, VRE

*combination reduce resistance Bacteriostatic +Statins: Rhabdomyolysis Norfloxacin: Topical Enzyme Inhibitors (AE) CI: Pregnancy

Gram +ve, C perfringens Conjuctivitis + Skin Infection Salmonella, Shigella UTi, Enteric Fever, Enterocolitis Res. Tuberculosis, Meningitis

Streptomycin Neomycin PSI Aminoglycosides Tobramycin Kanamycin Gentamicin Amikacin Synthetic Natural

Bind to 30s Interfere Proofreading +Abnormal Protein Bacteriocidal (*depends on conc)

Resistant Tuberculosis Gut Sterilization Gram ve (pseudomonas) Research (isolate bacteria) MRSA, Enterococci Multidrug-Res. Gram -ve Chronic Disease Ototoxicity Renal Failure

+ INH / EMB / PZA Topical

+Vancomycin: MRSA

Most Potent Acid Labile (-lactamase sensitive) Allergy Opp. Infections Diarrhoea ( with Amoxicillin) Rare: Hemolysis Nephritis Neurtoxicity Acid Stable

Penicillin G

Natural

Meningitis, Pneumonia, Syphilis Endocarditis (+Gentamycin) Oral Infections +-lactam Ring Bind to PBP X-transpeptidase Inhibit Petidoglycan Synthesis on Bact. Cell Wall Identify MRSA Anti-staphylococcal (Skin + Soft Tissue)

Penicillin V Methicillin Cloxacillin Penicillins CELL WALL SYNTHESIS INHIBITORS Oxacillin Ampicillin Amoxicillin BETA-LACTAMS Piperacillin Carbenicillin Ticarcillin Cephazolin Cephalexin Cefoxitin Cephalosporin Cefaclor Cefixime Ceftriaxone Cefepime Cefpirome Monobactam Carbapenems Aztreonam Imipenem Meropenem

Semi-Synthetic Penicillinase Res.

Extended Spectrum

Bite Wound Infections (ie. Bedbugs) Sinusitus, URT Infections Nosocomial Pneumonia Anti-pseudomonas

Less Diarrhoea Piperacillin: Most Potent +Tazobactam

1 Generation 2 Generation 3 Generation 4 Generation

th rd nd

st

Klebsiella sp, Surgical Chemoprophylaxis Bacteriocidal Bind to PBP X-transpeptidase Inhibit Petidoglycan Synthesis on Bact. Cell Wall Diverticulitis, Pneumonia (+CAP) Gonorrhoea Nosocomial Pneumonia (Pseudomonas) Gram ve, Penicillin allergic patients Wide Range Gram +ve Gram ve (except Chlamydia)

Allergic Hemolytic Anemia Thrombocytopenia Neutropenia -Liver Function Cross BBB Opp. Infection (AAD) Nausea + Vomiting Allergic CNS Effects Non-Toxic Highly Resistance to -lactamase

Clavulanic Acid Beta-Lactamase Inhibitors Sulbactam Tazobactam Vancomycin Others Bacitracin Strep. Pyogenes, Topical Antibiotics Bacterial Meningitis, Staph Brain Abscess Enteric Fever Chloramphenicol Bind to 50S X-Transpeptidation Intra-Abd Abscess (B fragillis): +Metronidazole Tetracycline Resistance: Cholera, Rickettsia Tetracycline Chlortetracycline Tetracycline Oxytetracycline Democlocycline Doxycycline Minocycline Trimethoprim Co-trimoxazole Sulfamethoxazol e Intermediate Long Acting 1 5 Short Acting Bind to 30S Inhibit the attachment of tRNA X-transcription Rickettsia, Psittacosis, Chlamydia Brucellosis, Cholera Lyme, Acne, Bronchitis + SIADH Psittacosis, Syphilis, Chlamydia + Malaria Chemoprophylaxis : Anthrax HIV: prophylaxis for P. carinii Bact: Travelers Diarrhoea, UTI Protozoa: Isosporiasis, Toxoplasmosis GI Disturbance Super-Infection Hepatic, Renal Toxicity Photosensitivity Vestibular Toxicity Impaired by Food+ (Ca, Dairy, Iron, Al) Cross Placenta CI: Pregnancy Cross Placental + BBB Highly Toxic Inactivated by Hepatic Glucoronyltransferase Bacteriostatic + cidal MRSA, Pseudomembranous Colitis +Gentamycin +Metronidazole Inactivate Beta-Lactamase Protect Antibiotics (from destroyed by B-Lactamase) Combined with Penicillin

GI Disturbance Opp. Infection Bone Marrow Aplastic Anemia Gray-Baby Syndrome

BROAD-SPECTRUM

Ind: Bacteristatic Comb: Bactericide

Nausea + Vomitting Skin Rash Stevens-Johnson

CI: Pregnancy