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Pcol Notes 2023
Pcol Notes 2023
DIRECT-ACTING INDIRECT-ACTING
BETA Agonists Reuptake
Non-Selective ALPHA Agonists DOPAMINE Agonists Releasers Inhibitors
(Catecholamines)
Metaraminol
Phenylpropanolamine
Pseudoephedrine
DRUGS FOR AUTONOMIC NERVOUS SYSTEM: Adrenergic Drugs
SYMPATHOLYTICS/ ADRENERGIC ANTAGONISTS
DIRECT-ACTING
With Intrinsic
With Membrane-
ALPHA Stabilizing Action With Mixed Alpha-1 and Enhances
BETA BLOCKERS Sympathomimetic
BLOCKERS (MSA) Beta Blocking Activity Nitric Oxide
Activity (ISAs)
Propranolol
CARDIOSELETIVE Carteolol Carvedilol Nebivolol
NON-SELECTIVE ALPHA-1 ALPHA-2 NON-SELECTIVE (BETA-1 BLOCKERS)
BETA BLOCKERS
Pindolol
Celiprolol Labetalol
Metoprolol
Phenoxybenzamine = Prazosin = Anti-HTN Yohimbine
IRREVERSIBLE Nadolol
Acebutolol
Labetalol
Celiprolol
Atenolol
Metyrosine Guanadrel Reserpine
Alfuzosin = Anti-
BPH
Acebutalol
Guanethidine
Nebivolol
Bretylium
DRUGS FOR AUTONOMIC NERVOUS SYSTEM: Cholinergic Drugs
CHOLINOMIMETICS/ CHOLINERGIC AGONISTS
DIRECT-ACTING INDIRECT-ACTING
(AChE inhibitors)
CHOLINE
ALKALOIDS
ESTERS
Aminoalcohols Carbamates Organophosphates
Non-selective Muscarinic- Muscarinic- Nicotinic- (Short-Acting) (Intermediate-Acting) (Irreversible, Long-Acting)
Non-selective
Choline Esters selective Selective Selective
Tx for Carbamate
Bethanechol Edrophonium Malathion
Acetylcholine Arecoline Muscarine Nicotine Myasthenia Gravis Insecticides
(Urecholine)
Nerve Gases
Methacholine Varenicline Neostigmine Aldicarb
(Sarin, Tabun, Soman)
Tacrine
Demecarium Methomyl
Donepezil
Galantamine
Rivastigmine
DRUGS FOR AUTONOMIC NERVOUS SYSTEM: Cholinergic Drugs
CHOLINOLYTICS/ CHOLINERGIC ANTAGONISTS
ANTIMUSCARINIC/ANTICHOLINERGIC AGENTS
NON-SELECTIVE
CNS-Acting Ophthalmic Respiratory Gastric GIT and Urinary
Atropine Antimuscarinics Antimuscarinics Antimuscarinics Anticholinergics Anticholinergics
Choline
Vesicular Uptake Exocytosis Cholinesterase
Reuptake
Inhibitor Inhibitor Reactivators
Inhibitor
Scopolamine Homatropine Ipratropium Pirenzepine Methscopolamine
Diacetyl
Monoxime
Benztropine Cyclopentolate Oxitropium Propantheline Hyoscine
ANTI-NICOTINIC AGENTS
Ganglionic Blockers Neuromuscular Blockers Trihexyphenidyl Tropicamide Dicyclomine Dicycloverine
(NN Blockers) (NM Blockers)
Atracurium Pancuronium
Cisatracurium Vecuronium
AUTACOIDS: Bradykinin, Eicosanoids, Serotonin, Histamine
BRADYKININ SEROTONIN
Receptor Location Effect Drugs
Drug PG Effect Use 5-HT 1B/1D Cerebral cerebral vasoconstriction -triptans (migraine headache)
Type blood (anti-migraine effect)
Misoprostol PGE-1 Cytoprotection •NSAID-induced ulcer Vessels
•Opening of Ductus Arteriosus
5-HT 2A/2B Smooth contraction of smooth Ergotamine (migraine headache)
Epoprostenol PGI-2 Vasodilation •Primary Pulmonary HTN muscles muscles Ergonovine (post-partum bleeding)
•Oxytosis (uterine Methysergide (prophylaxis of migraine)
contraction; opposite of Ketanserin (anti-HTN)
Dinoprostone PGE-2 Cervical •US-approved abortificacient tocolysis)
ripening •Bronchospasm
•Vasoconstriction Ritanserin (inhibit platelet aggregation)
Alprostadil PGE-1 Vasodilation (in •Erectile Dysfunction (male- Platelets
local penile assited suppository) Platelet aggregation
tissue)
5-HT 3 Chemorecept Emesis -setrons (Chemotherapu-induced N&V)
Latanoprost PGF-2α Reduced •Glaucoma or Trigger *Alosetron ( IBS-diarrhea)
(also intraocular *Off-label: eyelash growth Zone (CTZ)
Carboprost) pressure enhancer
5-HT 4 GI Tract Peristalsis Cisapride (partial)
Tegaserod (partial)
Prucalopride
^^ IBS-constipation
NOTE: Ergot Alkaloids are NOT autacoids. They only act on 5-HT receptors.
ERGOT ALKALOIDS:
1. Alpha Agonists = Methylergonovine
2. Alpha and 5-HT Agonist = Ergotamine
3. 5-HT Agonists = Methysergide
4. Other Alkaloids
1. Bromocriptine
2. Cabergoline
3. Perfgolide
4. Ergonovine
AUTACOIDS: Bradykinin, Eicosanoids, Serotonin, Histamine
HISTAMINE
AGONISTS ANTAGONISTS
Epinephrine H1 Antihistamines H2
Impromidine Antihistamines
Second
First Generation Cimetidine
Generation
Ethanolamine Ethylenediammine Alkylamine Piperazine Phenothiazine Piperidine Piperazine Piperidine Alkylamine Newer Agents Famotidine
Pyrilamine/
Diphenhydramine Chlorpheniramine Meclizine Promethazine Cyproheptadine Cetirizine Loratadine Acrivastine Bilastine Ranitidine
Mepyramine
Astemizole
Carbinoxamine
(withdrawn)
Orphenadrine
DRUGS FOR RHEUMATOLOGIC DISORDERS
ANALGESICS: NON-NARCOTICS
Paracetamol NSAIDs
Salicylic Acid Pyrazolone Indole Pyrrole Alkanoic True Phenyl Acetic Acid Oxicam Propionic Acid
Fenamates Celecoxib
Derivatives Derivatives Derivatives Acid Derivatives Acetates Derivatices Derivatives Derivatives
Aspirin Phenylbutazone Indomethacin Tolmetin Sulindac Ketorolac Mefenamic Acid Piroxicam Ibuprofen Etoricoxib
Meloxicam**
Diflunisal Dipyrone Aceclofenac Etodolac Meclofenamic Acid (preferentially Naproxen Parecoxib
selective to COX-2)
Magnesium Choline
Sulfinpyrazone Diclofenac Nabumetone Flufenamic Acid Keptoprofen Valdecoxib
Salicylates
Rofecoxib
Methyl Salicylate Flurbiprofen
(withdrawn)
Meloxicam **
(preferentially
selective to COX-2)
DRUGS FOR RHEUMATOLOGIC DISORDERS
ANALGESICS: NARCOTICS
OPIOID AGONISTS
Naltrexone
Meperidine
Nalorphine
Nalmefene
Levorphanol
Levallorphan
Fentanyl
DRUGS FOR RHEUMATOLOGIC DISORDERS
DISEASE-MODIFYING ANTIRHEUMATIC DRUGS (DMARDs)
NON-BIOLOGICALS
Chloroquine Aurothiomalate
Sulfpyridine
Hydroxychloroquine Auroglucose
5-aminosalicylate/
mesalamine Auranofin
BIOLOGICALS
Infliximab
*Route of Administration of Glucocorticoids:
•Systematic (IV, PO) = RA, SLE
•Local (Intrasynovial) = Osteoarthritis
Etanercept
DRUGS FOR RHEUMATOLOGIC DISORDERS
DRUGS FOR GOUT
st st
Colchicine Inhibits polymerization of 1 line for ACUTE Gout •Watery Allopurinol Inhibits Xanthine Oxidase/ 1 line for CHRONIC Gout
tubulin inhibition of diarrhea Xathine Oxidoreductase Purine analog
microtuble synthesis •Bloody
diarrhea
•Neuropathy
Febuxostat Inhibits Xanthine Oxidase/ Non-purine
Xathine Oxidoreductase
NSAIDs COX inhibition Indomethacin (Topical) -[recall
Ibuprofen NSAIDs S/E)
Pegloticase, Anti-inflammatory Uricase = not present In
*Do NOT give Aspirin, Rasburicase immunosupression mammals, converts uric acid to
Tolmetin, and Salicylates ALLANTOIIN (non-toxic
metabolite)
Glucocorticoids Anti-inflammatory Used NOT MORE THAN 5 •Cushing
immunosupression DAYS syndrome Penicillamine Enhance urinary secretion RISK: formation of RENAL
(especially if non-responsive Probenecid of uric acid (uricosuric URIC ACID STONES
to Colchicine and NSAIDs) Sulfinpyrazone agents) prevention: frequent
hydration
DRUGS FOR HEMATOLOGIC DISORDERS
DRUGS FOR COAGULATION DISORDERS: Anti-thrombotics
ANTICOAGULANTS
DIRECT INDIRECT
ANTICOAGULANTS ANTICOAGULANTS
Enoxaparin Dicoumarol
Lepirudin Apixaban
(withdrawn)
Dalteparin Phenprocoumon
Rivaroxaban
Bivalirudin (withdrawn)
Tinzaparin
Warfarin**
Argatroban
Fondaparinux
Photo Credit: Sir Crisfel Del Mundo
Danaproid
DRUGS FOR HEMATOLOGIC DISORDERS
DRUGS FOR COAGULATION DISORDERS: Anti-thrombotics
ANTIPLATELETS
Irreversible Reversible
Aspirin Dipyridamole
Epitifibatide
Ticlopidine Tigacrelor
Cilostazol
Abciximab
Clopidogrel
Tirofiban
Prasugrel
DRUGS FOR HEMATOLOGIC DISORDERS
DRUGS FOR COAGULATION DISORDERS: Fibrinolytics DRUGS FOR COAGULATION DISORDERS: Pro-thrombotics
FIBRINOLYTICS/
PRO-THROMBOTICS
THROMBOLYTICS
Reteplase K2 = Menaquinone
K3 = Menadione
DRUGS FOR HEMATOLOGIC DISORDERS
DRUGS FOR DYSLIPIDEMIA
•Most effective:
Atorvastatin increase HDL levels
Fenofibrate Ezetimibe
•T/E: Cholestyramine
Erythema/Flushing (Tx:
ASA, Ibuprofen)
•COMB. Prep:
Simvastatin +
Rosuvastatin Clofibrate Colestipol Ezetimibe (Vytorin)
Clozapine
FIRST GENERATION
Olanzapine
Loxapine
Poliperidone
-peridol -thix
Ziprasidone
Aliphatic Piperazine Piperidine
Molindone
Aripiprazole
Quetiapine
DRUGS FOR CENTRAL NERVOUS SYSTEM
DRUGS FOR MOOD DISORDERS: Depression, Bipolar Disorder
ANTIDEPRESSANTS
Tranylcypramine Sertraline
Lithium Valproic
Carbamazepine Antipsychotics
Carbonate Acid
Selegiline Citalopram
Escitalopram
DRUGS FOR CENTRAL NERVOUS SYSTEM
DRUGS FOR ANXIETY
Ramelteon
Alprazolam
Alprazolam
DRUGS FOR CENTRAL NERVOUS SYSTEM
DRUGS FOR SEIZURE
DRUG MOA T/E Notes
Carbamezepine Na Channel •T/E: Dose-related •DOC for
blocker Ataxia = loss of control of movement Trigeminal
Diplopia= loss of vision Neuralgia
ANTI-SEIZURE/ •Teratogenic (Spina Bifida) •Enzyme
inducer
ANTICONVULSANTS •Capable of
auto-induction
Phenytoin Blocks Na, K, •Most Common: Nystagmus •Fosphenytoin
Generalized Absence Atonic Myoclonic Status Acute and Ca •Dose-related (given as IM
Seizure Seizure Seizure Seizure Epilepticus Seizure conductance Ataxia = loss of control of movement and IV)
Diplopia= loss of vision
•Cosmetic Changes
Valproic Ethosuximide Clonazepam Lorazepam Diazepam Gingival hyperplasia, Hirsutism
Valproic •Idiosyncratic
Acid Acid SJS, Blood dyscrasias
•Teratogenic: Fetal Hydantoin Syndrome
Valproic acid Valproic Clonazepam
Topiramate Acid Valproic Acid •Increases •Hepatoxicity (avoid in <2 yrs old) •Enzyme
(more recent)
GABA •Teratogenic: Spina bifida) inhibitor
concentration
by stimulating
Topiramate
Glutamic Acid
Lamotrigine decarboxylase
•Blocks Na and
Ca conductance
Lamotrigine
Lamotrigine Na channel
blocker
Ethosuximide T-type Ca
Channel blocker
Topiramate Na and Ca
channels
blocker
DRUGS FOR CENTRAL NERVOUS SYSTEM
DRUGS FOR PARKINSON’S DISEASE
ANTI-PARKINSONIAN DRUGS
Non-Ergot
Tolcapone Selegiline Ergot Derivatives Biperiden
Derivatives
ANESTHETICS
General Local
Anesthetics Anesthetics
Halothane
Methoxyflurane
DRUGS FOR RESPIRATORY DISORDERS
DRUGS FOR COLDS DRUGS FOR COUGH
Bromhexine Butamirate
Codeine
Citrate
Carbocisteine Noscapine
Dextromethorphan
DRUGS FOR RESPIRATORY DISORDERS
DRUGS FOR BRONCHOSPASTIC DISEASES
BRONCHODILATORS
Terbutaline Formoterol
ANTI-INFLAMMATORY
Metoproterenol
Anti-Leukotrienes Corticosteroids Anti-IgE
Picaterol/
Pirbuterol LTD-4 receptor Inhaled Systemic ORAL Systemic
LOX inhibitor PARENTERAL Omalizumab
Antagonists Corticosteroids Corticosteroids
Corticosteroids
Triamcinolone Methylprednisolone
ENDOCRINE DRUGS
HYPOTHALAMIC AND ANTERIOR PITUITARY GLAND HORMONES AND AGENTS
GROWTH HORMONE
GONADOTROPIN RH
GH Deficiency GH Excess
Cabergoline Bromocriptine
ENDOCRINE DRUGS
OXYTOCIN VASOPRESSIN
Vasopressor
Central DI Nephrogenic DI Demeclocycline Receptor
To stimulate milk let-down Tx/Prevention of post- Antagonists
partum hemorrhage
THYROID HORMONES
THYROID HORMONES
HYPOthyroidism HYPERthyroidism
Carvedilol Ipodate
ENDOCRINE DRUGS
ADRENOCORTICAL HORMONES
ADRENOCORTICAL HORMONES
Glucocorticoids Mineralocorticoids
Eplerenone
ENDOCRINE DRUGS
GONADAL HORMONES
ESTROGEN PROGESTIN
Natural Synthetic
Endogenous 19- 19-Ethyl-19-
Progesterone
form: Testosterone Nortestosterone Nortestosterone
Derivative
Progesterone Derivatives Derivatives
E1: Estrone Steroidal Non-Steroidal
Methoxyprogesterone
acetate ( IM Depo-
Provera) Dimethylsterone Levonorgestrel Desogestrel
Mestranol Diethylstilbestrol
E2: Estradiol (Major (banned)
secretory form)
Norethindrone Norgestimate
Quinestrol Methallenestril
ENDOCRINE DRUGS
GONADAL HORMONES
DRUGS FOR
CONTRACEPTION FERTILITY DRUGS
Injectables: IM Depo-
provera)
Monophasic TESTOSTERONE Urofollitropins (FSH)
Intradermal implants
Biphasic Etonorgestrel (Implanon) Testosterone Analogues Testosterone
(Anabolic Steroids) Antagonists
Finasteride Flutamide
Danazol
Bicalutamide
ENDOCRINE DRUGS
INSULIN
Insulin Zinc
Suspension
ENDOCRINE DRUGS
Glibenclamide/
Acetohexamide
Glyburide
DRUGS FOR CARDIOVASCULAR DISEASES: Hypertension
DIURETICS
NATRIURETICS AQUARETIC
Bumetanide
Chlorothiazide Indapammide
Dorzolamide Eplerenone Triamterene
Metolazone
Dichorphenamide
CLASS SITE OF ACTION MOA T/E
Carbonic Anhydrase Proximal Convoluted Inhibits Carbonic Anhydrase •Metabolic acidosis ( due to increase carbonic acid in blood)
Inhibitors Tubule (PCT)
Loop Diuretics (aka High- Thick ascending loop (TAL) Inhibits Na-K-2Cl co-transporter •Electrolyte Imbalance (reduced levels)
ceiling diuretics) •Sulfa-related reactions (SJS, Hemolytic Anemia)
•Ototoxicity (ethacyrynic acid
•HyperGLU (Glycemia, Lipidemia, Uricemia)
Thiazide Diuretics Distal Convoluted Tubule Inhibits NaCl co-transporter •Electrolyte Imbalance (reduced levels)
(DCT) •Sulfa reactions
•HyperGLUC Glycemia, Lipidemia, Uricemia, Calcium)
K-Sparing Diuretics Collecting Duct Aldosterone Antagonism (S, E) •Hyperkalemia
Epithelial Na Channel Inhibitor •Spironolactone ( anti-androgen effects like gynecomastia)
(ENAC inhibitors) (A, T) •Triamterene: Increased risk of renal stone formation
Aquaretic (Mannitol) PCT, TAL (Loop of Henle) Creates an osmotic gradient in •Dehydration
H2O-permeable sites (PCT, TAL) •Hypovolemia
•HYPERnatremia (due to low blood volume)
DRUGS FOR CARDIOVASCULAR DISEASES : Hypertension
SYMPATHOPLEGICS
SYMPATHOPLEGICS
Centrally-Acting: Peripherally-Acting:
Ganglionic Blockers Alpha Blockers Beta Blockers
Alpha-2 Agonists Adrenergic Neuronal
Blockers
Reserpine Trimethaphan
Methyldopa
Guanethidine
Mecamylamine
Guanfacine
Guanedrel
Guanabenz
Bretyllium
DRUGS FOR CARDIOVASCULAR DISEASES: Hypertension
DIRECT VASODILATORS
MECHANISMS OF VASODILATION
Tezosentan
Na
Nitroprusside Diazoxide
DIRECT VASODILATORS
ANGIOTENSIN ANTAGONISTS
SYMPATHOPLEGICS
Aliskiren -sartan
Acute ACEi’s Rest are
(non-prodrug) Prodrugs
Captopril
Lisinopril
Enalaprilat
DRUGS FOR CARDIOVASCULAR DISEASES: Angina Pectoris
ANTI-ANGINALS
ANTI-ANGINALS
Calcium Channel
Nitrovasodilators Beta-Blockers
Blockers
Cardiac Endothelin
Beta-1 Agonists Bipyridines ACEIs/ARBs Diuretics Vasodilators Beta Blockers
Glycosides Antagonists
(PDE-3 inh)
Hydralazine
Digoxin Dobutamine Bosentan Bisoprolol
+ISDN
Inamrinone
Metoprolol
Digitoxin Dopamine Nesiritide Tezosentan
succinate
Milrinone
Carvedilol
Nebivolol
DRUGS FOR CARDIOVASCULAR DISEASES: Arrhythmia
ANTI-ARRHYTHMICS
Class I: Sodium Class II: Beta- Class III: Potassium Class IV: Calcium- Miscellaneous
Channel Blockers Blockers Channel Blockers Channel Blockers Agents
(Non-DHP)
Sotalol (only
Criterion IA IB IC Amiodarone Dronedarone Class III Beta- Miscellaneous Digoxin
+
blocker)
Na Blockade Moderate Weak Strong Diltiazem
Adenosine
Action Prolong Shorten No effect Bretyllium
Potential
Duration Verapamil Magnesium
Sulfate
Examples Disopyramide Tocainide Moricizine
Quinidine Mexiletine Flecainide Dofetilide
Procainamide Lidocaine Propafenone
Phenytoin Encainide
Ibutilide
DRUGS FOR GASTROINTESTINAL DISORDERS
DIARRHEA
Diphenoxylate Cholestyramine
Colestipol
Loperamide
Colesevelam
CONSTIPATION
Nizatidine Misoprostol
Pantoprazole Nitroimidazole
Bismuth
Subsalicylate
Rabeprazole Potassium
DRUGS FOR GASTROINTESTINAL DISORDERS
DRUGS FOR IRRITABLE BOWEL DRUGS FOR INFLAMMATORY BOWEL SYNDROME
SYNDROME
Antimuscarinics Scopolamine
Corticosteroids Dexamthasone
Medroxyprogesterone
Acetate (Depo-provera) Gonadorelin Fulvestrant Tamoxifen Anastrozole
Levonorgestrel
TESTOSTERONE-BASED
Megestrol
DRUGS CORTICOSTEROIDS
Norgestrel Androgen 5-alpha-
GnRH
Receptor reducatase
Antagonists
Norgestimate
Blockers Inhibitors
Prednisone Methylprednisolone
Flutamide Abarelix Finasteride
Progesterone
Nilutamide Degarelix
Ganirelix
ANTI-CANCER AGENTS
Cytotoxic Agents
AlkylatingAgents
Agents Topoisomerase Inhibitors Antitumor Antibiotics
Alkylating
Dactinomycin
Mitomycin Bleomycin
Anthracyclines (Actinomycin D)
Mechlorethamine Camptothecins Podophyllotoxin
Derivatives
Cyclophosphamide
Irinotecan Doxorubicin
•Phospharamide Mustard
•Acrolein Etoposide
Topotecan Daunorubicin
Busulfan
Teniposide
Carmustine and Idarubicin
Lomustine
Altretamine Epirubicin
Procarbasine and
Dacarbazine
Mitoxantrone
Temsolomide
Cisplatin, Carboplatin,
and Oxaplatin
ANTI-CANCER AGENTS
Cytotoxic Agents
Cladribine
ANTI-CANCER AGENTS
Targeted Therapy
TARGETED THERAPY
Regorafenib
Ramucirumab
•EGFR = Epidermal growth factor receptor
•VEGFR = Vascular Endothelial Growth Factor
Receptor
•ALK = Anaplastic Lymphoma Kinase
•BCR-ABL = Breakpoint Cluster Region – Abelson
•B-RAF = type of proto-oncogene
•mTOR = Mammalian target of rapamycin
•PD-1 = Programmed Cell Death Protein 1
•CD20 = Cluster of Differentiate 20
ADDITIONAL INFO
(No particular order)
SYMPATHETIC NS PARASYMPATHETIC NS
Storage •Reserpine = inhibits vesicular uptake of NE Vesamicol = inhibits vesicular uptake of Ach
5-HT1B/1D Cerebral blood Vessels cerebral vasoconstriction (anti- -triptans (migraine headache)
migraine effect)
Inhaled Corticosteroids
Budesonide
Type MOA Examples Fluticasone
Mucoregulators Increases H2O portion of bronchial Ambroxol Triamcinolone
gland allows easier expectoration Bromhexine
Carbocisteine
POISON ANTIDOTE
Acute Lead Poisoning (<24 Chronic Lead Poisoning Paracetamol N-acetyl-cysteine
hrs): (>3 mos): Atropine -stigmines
Encephalopathy Burton’s lines
Milky vomitus, Anemia Organophosphate 1st 24 -48 hrs: Atropine and Pralidoxime
Melena Developmental delay >48 hrs: Atropine
Wrist drop and foot drop
Warfarin Vitamin K
Opioid Naloxone
Pro-aggregants Anti-aggregants
Benzodiazepine Flumazenil
Platelet-derived Endothelial cell-derived
Stimulated: CLOTTING Stimulated: BLEEDING Digoxin Lidocaine IV (Digoxin-Induced Ventricular
Inhibited: BLEEDING Inhibited: CLOTTING Tachycardia)
Digifab or Digibind (Digoxin toxicity with no
Examples: Examples: arrhythmia)
•ADP •cAMP Phenytoin (Digoxin-induced Tachyarrhythmia)
•Serotonin •PGE
•TXA2 •PGI2 Beta blockers Glucagon
ANTIBIOTICS SPECTRUM OF ACTIVITY
AGENT EFFECT RESCUE DRUG
Cisplatin, Nephrotoxicity Amifostine,
Carboplatin hydration
Cyclophosphamide, Hemorrhagic cystitis (due MESNa
Ifosfamide to accumulation of
acrolein)
Doxorubcicin Caridotoxicity Dexrazoxane
Irinotecan, Diarrhea Hydration
Topotecan
Busulfan, Pulmonary fibrosis Supportive
Bleomycin treatment only
CLASS II CLASS I
PhenyBINGGE DilTheoMet ProParaVer
High Vd Low Vd
Phenytoin, Bicalutamide, Diltiazem, Theophylline,
PERMEABILITY
SOLUBILITY
Zero Order Kinetics First Order Kinetics
Phase I : Functionalization Phase Phase II : Conjugation Phase
→ Amount is fixed → Amount is not fixed
→ Rate is fixed → Rate is not fixed Unmasking polar functional group → Addition of polar functional group
→ Independent on concentration → Dependent on concentration
(not proportional (proportional)
•Oxidation •Glucuronidation
→ Elimination for certain drugs : → Elimination for majority of drugs •Reduction •Amino acid conjugation
Zero WHATTS Power •Hydrolysis •Glutathione conjugation
•Warfarin •Sulfation
•Heparin •Acetylation
•Aspirin, Alcohol •Methylation
•Theophylline
•Tolbutamide
•Salicylates
•Phenytoin