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Pharmacology Revision E6.5 (Medmutant - Xyz)
Pharmacology Revision E6.5 (Medmutant - Xyz)
Pharmacology Revision E6.5 (Medmutant - Xyz)
Types of drugs :
Types of drugs Description
Orphan drug Used in the treatment of rare diseases.
Essential drugs Satisfying the health care need of majority of the
population.
Features :
a. Single molecule (Not FDC).
b. Safe.
c. Easily available.
d. Affordable.
Prescription drugs Belonging to schedule H class.
Given only after producing prescription.
Spurious drugs Not producing adequate response due to inadequacy in
the drug.
Misbranded drugs Wrongly labelled drug.
Adulterated drugs Drugs with additional unwanted component.
Types of tablets/capsules :
Plasma concentration
Time
Concentration (C)
the systemic circulation.
Ranges from 0-1 (0 = 0% ; 1 = 100%).
Only route with 100% : IV.
Tmax
Time (T)
Depends on : Cmax : Maximum concentration of drug
• First pass metabolism. that can be achieved.
• Absorption. Tmax :
• Time taken for Cmax.
• Marker for rate of absorption.
AUC B C D
Concentration (C)
Oral A
AUC
IV
Time (T)
Rate of absorption : A > B > C > D.
(AUC : Area Under Curve).
----- Active space ----- Pgp substrates Pgp inducers Pgp inhibitors (“VACINE”)
V : Verapamil
Digoxin Enzyme inducers. A : Amiodarone
Protease inhibitors. Eg. : C : Cyclosporine
Loperamide Rifampicin. I : Itraconazole
Bile acid Quinidine N : Nifedipine
E : Erthyromycin/Clarithromycin
Pharmacokinetics : Distribution 00:26:10
Dialysis :
Ineffective against drugs with high VD : “BAD-DOC”.
Drug Antidote
Benzodiazepines Flumazenil
Beta blockers Glucagon
Amphetamine Ammonium chloride
Digoxin Digibind
- -
Opioids Naloxone
Organophosphates Atropine
Calcium channel blockers Calcium gluconate
Mechanism of excretion :
Filtration Tubular secretion
20% of excretion 80% of excretion
Excretes only free drugs (Not plasma Excretes both free and plasma protein
protein bound) bound drugs.
Formulae :
Rate of drug elimination (mg/h) = PC × CL.
PC : Plasma concentration.
Infusion/Dosing rate (To acheive steady
CL : Clearance.
state) = PC × CL.
t : Time.
Maintenance dose = PC × CL× t. VD : Volume of Distribution.
t1/2 = 0.693 × VD/CL Ke (Elimination constant) = VD/CL.
t1/2 = 0.693/Ke.
Zero order Vs. First order kinetics : ----- Active space -----
Pharmacodynamics 00:00:09
Affinity Efficacy
Terms Definition
• Tendency of a drug to bind to a target.
Affinity
• Dose required to bind to target.
• Maximum clinical effect produced by a drug.
Efficacy
• Effect produced (Most important clinically).
• Relative dose of a drug required to produce a particular effect.
Potency • Potency a 1/Dose.
Response Response
0
Log dose
ED50 TD50 LD50 Log Dose
ED50 : Dose required to produce effect in Efficacy : B > A > C. Taller graph Higher
50% population. Marker of potency. Efficacy.
TD50 : Dose required to produce toxicity in Potency : A > B > C. Lesser dose More
50% population. marker of toxicity. potent.
LD50 : only in animals. Dose required to kill Affinity : A > B (Affinity can be compared
50% animals. marker of toxicity. only if the drugs act on same
target Only if DRCs are parallel).
Therapeutic window/range :
MTC
Plasma Therapeutic
Concentration window
MEC
Time
• MEC (Minimum effective concentration) : Effect seen only beyond MEC.
• MTC (Minimum toxic concentration) : Toxicity begins beyond MTC.
• Therapeutic range = between MEC & MTC.
A : Full agonist
• Full agonist : Maximal effect (+1).
B : Partial agonist
• Partial agonist : Submaximal effect (+1 to 0).
• Antagonist (m/c) : No effect (0). C : Antagonist
Types of antagonism :
Types Examples
1. Physical/pharmacokinetic Alcohol : Charcoal.
2. Chemical Heparin : Protamine sulphate.
Iron : Desferrioxamine.
3. Physiological Histamine (H1) → Bronchoconstriction.
Adrenaline (β2) → Bronchodilation.
Trials 00:33:39
Exception for normal healthy volunteers in Phase 1 : Trial for anti-cancer &
anti- HIV drugs.
Therapeutic Exploratory Trial. 100-500 patients, Unicentric.
II Dose range. 2-3 years.
Safety. Randomized Controlled Trial
Determine Efficacy. (RCT).
Therapeutic Confirmatory Trial. 500-3000 patients, Multicentric.
III Safety. 3-5 years.
Confirm Efficacy. RCT/RUCT.
Drug is approved by CDSCO/FDA & marketed..
Pharmacovigilance :
ADR reporting software : Vigiflow.
National coordinating centre : IPC ghaziabad (Forms conclusive report).
CDSCO Delhi : Bans the drug based on the report.
International pharmacovigilance center : Uppsala, Sweden.
CYP450 polymorphism :
• CYP2C19 → Effect of clopidogrel.
• CYP2C9 → Variable effect of warfarin.
• CYP2D6 → Toxicity of antidepressants/antipsychotics.
Note :
• “-fenacin” drugs : Selective M3 blockers.
• Trospium : Quaternary amine, no BBB crossing.
Most specific drug for OP poisoning : Pralidoximes (Acetyl Esterase reactivator). ----- Active space -----
Most specific sign of Atropinisation : Decreased respiratory secretions.
Beta blockers :
Effect of catecholamines on HR :
Dale’s phenomenon :
(α1)
BP
(β2) Time
Administration of
drug
- Dale : Biphasic pattern
Epi + β blocker (Re-reversal of Dale)
Epi + α blocker (Vasomotor reversal of Dale)
↑ uveoscleral
Bimatoprost (latanoprost). • Cystoid macular edema
outflow
No response • C/I : Uveitis/ Herpetic keratitis
→ add beta (prostaglandins ↑ inflammation)
blockers
Timolol, • Timolol : NLD obstruction d/t
Metipranolol, 2nd line in stenosis
Beta blockers
outflow
line)
1. Rx of SVT/PSVT :
AV node blockers (Rate control) : ABCD drugs.
Drug Route Uses C/I
DOC for an acute C/I in COPD, asthma
Adenosine I.v attack SVT (Rapid I.V & atrial fibrillation
push). (Induces AF).
C/I in COPD &
Beta blockers I.v & oral
bronchial asthma.
Calcium channel
blockers (CCB) :
I.v & oral DOC for SVT in COPD
• Verapamil
/asthma Pt.
• Diltiazem
Digoxin Oral
In acute attack : Use I.v drugs (Adenosine > Beta blockers > CCB).
In long term Rx : Use oral drugs (Beta blockers > CCB > Digoxin).
----- Active space ----- Acute heart failure Chronic heart failure
DOC for pulmonary edema : 2. Omapatrilat : Neprilysin inhibitor +
Furosemide ACE inhibitor.
no response Other drugs : SHIVA Beta
IV Nitroglycerine 3. Spironolactone.
(Reduces preload) 4. SGLT 2 inhibitors.
no response 5. Hydralazine + Isosorbide dinitrate.
BNP analogue 6. Ivabradine.
(IV Nesiritide) 7. Vericiguat.
Nesiritide is metabolized by neutral 8. ACE inhibitors/ARB.
endopeptidase (Neprilysin). 9. Beta-blockers.
----- Active space ----- Antianginal drugs MOA (In stable angina)
Ivabradine
risk of AF & luminous phenomena Funny channel inhibition
(seeing colorful halos).
Nicorandil K+ channel opener
Fasudil Rho kinase inhibitor
Trimetazidine PFOX inhibitor
Statins, Aspirin, ACE inhibitors mortality in stable angina.
Amiodarone:
Mnemonic : Potassium channel blocker makes liver, nerve and skin toxic
• Pulmonary fibrosis
• Cornea Verticillata (Whorl like deposits in cornea)
• Blue colored skin (Ceruloderma, on sun exposed areas)
• Myocarditis
• Liver toxicity
• Neurotoxicity
• Alpha receptor block : Causes hypotension
• Photosensitivity (Brown skin : on sun exposed areas)
• Thyroid (Hypothyroidism > Hyperthyroidism)
S/E of CCB :
• Headache
• Constipation (Only verapamil)
• Ankle edema (Prevented by ACEi/ARB)
• AV block (Only verapamil & diltiazem)
Verapamil & diltiazem should not be given with beta blockers.
Hypertriglyceri-
demia
Bile acid binding Hyperchloremic
Inhibit enterohepatic Add on to statins
resins : alkalosis
Cholestyramine circulation of bile acid,
Preferred in pregnan- GI upset & Ab-
Colestipol LDL. cy & children. sorption of other
Colesevelam
drugs (Minimum
with colesevelam)
Triglyceride rich
Hypertriglyceridemia
VLDL synthesis/se-
Icosapent cretion by liver.
Add on to statins
Inhibits platelet ag-
( CVS mortality).
gregation
Rosuvastatin 5 - 10 mg Rosuvastatin 10 - 20 mg
& &
Atorvastatin 10 - 20 mg Atorvastatin 40 - 80 mg
Rx of Hypertriglyceridemia :
Assess the risk of ASCVD
Absent Present
1. Diuretics
Drug class MOA Uses
• Acetazolamide : DOC in acute
mountain sickness.
Carbonic anhy- Block carbonic
• Acetazolamide/Dichlorphenamide:
drase inhibitors anhydrase in PCT.
Familial hypokalemic periodic
paralysis.
• Blocks Na/K/2Cl DOC in (renal/cardiac) edema.
pump in thick • Furosemide : DOC in cardiogenic
ascending limb. pulmonary edema.
Loop diuretics • Indirect vasodila- • Torsemide : Longest acting.
tors : • Bumetanide : Most potent.
Prostaglandins. • Ethacrynic acid : Most ototoxic.
NSAIDs → effect. Most effective if GFR< 40.
Uses : First-line in mild/moderate
• Blocks Na/Cl
HTN, add-on drug in edema mx.
cotransporter in
• Chlorthalidone : Longest acting,
DCT.
preferred in HTN mx.
• Direct vasodila-
Thiazides • Chlorothiazide : Shortest acting.
tors :
• Indapamide : Predominantly he-
• Open K channels,
patic excretion.
so they are ef-
All others → Renal excretion.
fective in HTN.
Metolazone : Effective in GFR <40.
K sparing di-
uretics
Aldosterone DOC in cirrhotic edema, resistant
Spironolactone,
antagonist. HTN.
Eplerenone
Carbonic
Loop K sparing Osmotic
anhydrase Thiazides
diuretics diuretics diuretics
inhibitors
Hypo/hyper-
Hypokalemia Hypokalemia Hypokalemia Hyperkalemia
kalemia
Metabolic Metabolic Metabolic Metabolic Hypo/hyper-
acidosis alkalosis alkalosis acidosis natremia
↓ Mg ↓ Mg Gynaecomastia
Renal stones ↑ Glucose ↑ Glucose (d/t spironolac-
↑ Uric acid ↑ Uric acid tone)
Pulmonary
Hyperam-
edema
monemia
↓ Ca2+ ↑ Ca2+ (even though
(C/I in liver
it is used as
cirrhosis)
DOC for cer-
Hypersensi- Cause oto-
ebral edema)
tivity; bone toxicity : C/I Worsens DM,
marrow sup- with amino- gout
pression glycosides
Disorders DOC
1. DOC : Riluzole.
2. If not responsive, Edaravone.
ALS 3. Newer agents :
• Sodium phenylbutyrate taurursodiol.
• Tofersen.
1. DOC : Cholinergics (Donepezil/rivastigmine/
galantamine).
2. Add memantine (NMDA receptor blocker) in
Alzheimer’s disease
mod-to-severe cases.
3. Newer agents : β amyloid blockers
(aducaNumab, lecaNemab) in mild cases.
RP
5HT 1B/1D (Triptan) CG
CGRP
CGRP receptor
Vasodilation in meningeal
blood vessels
Disorders DOC
Narcolepsy Modafinil
Insomnia :
1. DOC : Ramelteon (lesser dependence, less effective).
Sleep induction, jet lag
2. Zolpidem (If non-responsive).
1. DOC : DORA (dual orexin receptor antagonist) :
Sleep maintenance Suvorexant, daridorexant.
2. Zolpidem (If non-responsive).
Disorders DOC
Opioid toxicity DOC : Naloxone
• To ↓ withdrawal symptoms : Methadone,
Opioid dependence :
Buprenorphine
• To prevent relapse : Naltrexone.
Labour analgesia Morphine > Pethidine
Opioid induced constipation Methylnaltrexone
Postoperative ileus Alvimopan
Postanaesthetic chills Pethidine/Tramadol (MOA: α2 agonist)
Note : Tolerance to constipation, convulsions, and miosis is not seen with opioids.
New agents :
• Rett syndrome : Trofinetide.
• Fredrich’s ataxia : Omaveloxolone.
EPS Treatment
Akathisia (M/C) : Restlessness. 1. DOC : Beta blockers.
2. Add on : Benzodiazepines.
Side effects
Withdrawal symptoms
(d/t Mu receptors)
M Miosis Symptoms d/t withdraw-
U Urine retention al are opposite those d/t
S Sedation Mu receptor stimulation
C Constipation, Convulsion
A Analgesia
R Respiratory depression
I Increased muscle rigidity
N No bile flow – Contraction of sphincter of Oddi
E Euphoria
Note : Opioids are no longer C/I for pain management in biliary colic.
----- Active space ----- Cell Wall Synthesis Inhibitors : Site of action 00:06:30
1. Fosfomycin.
2. Cycloserine.
3. Bacitracin.
4. Vancomycin (inhibit
transglycosylation).
5. β lactams.
Antibiotic DOC in
• Atypical pneumonia : Chlamydia, mycoplasma, legionella.
• Campylobacter.
Azithromycin
• Cholera in children.
• Cholera and chlamydia in pregnancy.
• Listeria meningitis.
Ampicillin • Enterococcus faecalis endocarditis (Along with
gentamicin).
• Gonorrhea.
• Typhoid (Note : Oral DOC in typhoid → Cefixime).
Ceftriaxone (IV) • Haemophilus influenzae meningitis.
• Empirical treatment of meningitis.
• Infections of E. coli, Klebsiella & Providencia.
Ceftazidime Pseudomonas (Gentamicin is added in severe infections).
• Extended spectrum β lactamase producing organisms.
• Serratia.
• Acinetobacter.
Carbapenems • Enterobacter.
Note : Imipenem is metabolized by renal dehydropeptidase
and is combined with cilastatin, a renal dehydropeptidase
inhibitor.
• Ototoxicity (Irreversible).
Auditory : Amikacin.
Aminoglycosides
Vestibular : Streptomycin.
• Neuromuscular toxicity.
C/I : Pregnancy.
• Motilin receptor stimulation :
Hypertrophic pyloric stenosis.
Diarrhea.
Erythromycin
• Skeletal muscle weakness.
• QT prolongation.
• Cholestatic jaundice.
• Photosensitivity.
• QT prolongation.
• Rash.
Fluoroquinolones
• Seizure.
• Tendinitis, tendon rupture (Increased risk is seen in
elderly, renal failure and steroid use).
• Bone marrow suppression.
• MAO inhibition.
Linezolid • Mitochondrial toxicity :
Optic neuritis.
Lactic acidosis.
• Pseudomembranous enterocolitis (3rd generation
Beta lactams cephalosporins > amoxicillin).
• Hypersensitivity.
Cefoperazone,
moxalactam, • Disulfiram like reaction.
cefamandole, • Hypoprothrombinemia.
cefotetan
Imipenem • Seizures.
• Kernicterus after birth.
• Acute intermittent porphyria.
• Methemoglobinemia.
Sulphonamides
• Rash.
• Bone marrow suppression.
• Crystalluria.
Entry inhibitors
CD4 inhibitor GP 120 inhibitor CCR5 inhibitor GP 41 inhibitor
Ibalizumab (IV). Fostemsavir. Maraviroc. Enfuvirtide (S/c).
Active against HIV-1. Active against HIV-1. Active against Fusion inhibitor.
HIV-1 & 2.
Note : All antiretroviral drugs are given by oral route except ibalizumab and
enfuvirtide.
Protease inhibitors
Metabolized by CYP3A4 (Except Nelfinavir → metabolized by CYP2C19).
Enzyme inhibitors of CYP3A4.
Common S/E :
• Dyslipidemia.
• Hyperglycemia.
• Lipodystrophy.
• Lopinavir (LPV).
• Ritonavir :
Most potent enzyme inhibitor.
Used as a booster drug (E.g : LPV/r).
• Atazanavir : Does not cause dyslipidemia.
• Indinavir : S/E → Renal stones.
Pharmacology Revision • v1.0 • Marrow 6.5 • 2023
50 06 Pharmacology www.medmutant.xyz
Nematodes DOC
Roundworm.
Whipworm.
Hookworm. Albendazole.
Enterobius vermicularis.
Trichinella spiralis.
Ivermectin :
Strongyloides. MOA : Produces tonic paralysis by
Onchocerca volvulus. stimulating glutamate sensitive
chloride channels.
Diethylcarbamazine (DEC).
Loa loa.
Note : Ivermectin + DEC + Albendazole
Filariasis.
regimen is used to treat filariasis.
Drancunculiasis. Metronidazole.
Cestodes DOC
Neurocysticercosis.
Albendazole.
Echinococcus.
Intestinal Taenia solium.
Praziquantel
Taenia saginata.
MOA : Produces spastic paralysis by
Hymenolepis nana.
stimulating calcium channels.
Diphyllobothrium latum.
Pharmacology Revision • v1.0 • Marrow 6.5 • 2023
52 06 Pharmacology www.medmutant.xyz
Malaria
Chloroquine (S/E : Bull’s eye maculopathy, corneal deposits).
Uncomplicated
(+)
vivax malaria
Radical cure with : Primaquine for 14 days (Or) Tafenoquine
once.
Uncomplicated
falciparum • Artemisinin combination therapy (ACT).
malara and • Artesunate + Sulfadoxine + Pyrimethamine.
chloroquine • Artemether + Lumefantrine (Preferred in North
resistant vivax Eastern Indian states).
malaria
Severe
IV Artesunate : Most potent and fastest acting
falciparum
schizontocidal drug.
malaria
Liver.
Organ of
Liver. (Safest drug in Liver. Kidney.
excretion
renal failure).
Note :
• Purpura and pulmonary syndrome are indications to discontinue rifampicin
forever.
• Order of hepatotoxicity : Pyrazinamde > Isoniazid > Rifampicin.
Drugs of choice :
Brain tumor :
TOC refers to treatment regimen.
Temozolomide.
Head and neck
cancer : Cisplatin.
Esophageal : TOC : Cisplatin +
Cisplatin. 5FU.
TOC : Cisplatin
+ 5FU. Lung Cancer :
Cisplatin.
Liver :
Sorafenib. Gastric cancer :
Cisplatin.
TOC : Cisplatin +
Pancreas cancer : 5FU.
Gemcitabine.
Colorectal cancer :
5 Fluorouracil.
Kidney : TOC : FOLFOX/ FOLFERI
Pembrolizumab. 5 FU + Oxaliplatin/
Irinotecan + Folinic
acid ( Leucovorin).
Hematology
Leukemia Lymphoma
No response
Daunorubicin.
Dasatinib
Nilotinib (2 nd gen).
Bosutinib
No response
T- 315- I mutation
Note : The drugs used in Rx of CML are BCR-ABL Tyrosine kinase inhibitor →
Blocks the enzymatic site.
Others :
1. Olaparib : PARP blocker (Poly ADP Ribose polymerase) → Rx of Breast Ca.
2. Bortezomib : Proteazome inhibitor → Rx of Multiple Myeloma.
3. Sonidegib : Hedgehog pathway blocker.
4. Retinoic acid : DOC for Promyelocytic leukemia.
5. Aspariginase : Rx of ALL.
Note :
Side effects of Asparaginase :
• Hyperglycemia. • Hypercoagulation. • Hypersensitivity.
• Hyperlipidemia. • Hemorrhage.
1. PD 1 Blockers :
Nivolumab Pembrolizumab
Mnemonic : Nivea CREAM Hydration. Mnemonic : PEMBROLI.
• Non small cell lung Ca. • Primary mediastinal B-cell
• Colorectal Ca. lymphoma.
• RCC, Urothelial cancer. • Endometrial and Cervical Ca.
• Esophageal Ca, Gastric Ca. • Melanoma, Merkel cell cancer.
• Adjuvant Rx. • Breast Ca (triple -ve).
• Melanoma, Mesothelioma. • RCC, Urothelial Ca.
• Head and neck Ca, Hodgkin’s • Oesophageal, Oral and Gastric
disease. carcinoma.
• Liver Ca, Lung Ca, Hodgkin’s
lymphoma.
• Intestinal CA (Colorectal).
2. PD-L1 Blocker :
Durvalumab Avelumab Atezolizumab
Mnemonic : Dura BL Mnemonic : Avail RUM Mnemonic : Ate LAMB
• Biliary tract Ca. • RCC. • Ca Liver, Ca Lung (non
• Liver Ca / Lung • Urothelial cancer. small cell).
Ca (non small cell/ • Merkel cell • Alveolar sarcoma.
small cell). carcinoma. • Melanoma.
• Breast Ca (triple -ve).
Ipilimumab
Mnemonic : IP MEN Like Chinese Restaurant.
• Melanoma, Mesothelioma.
• Esophageal Carcinoma.
• Non small cell lung Carcinoma.
• Lung Carcinoma.
• Colorectal carcinoma.
• RCC.
Endocrinology 00:45:04
Antidiabetic drugs :
Note : Drugs which cause Hypoglycaemia → Insulin > drugs which cause in-
crease in insulin release.
GnRH agonist :
GnRH agonist :
• Goserelin.
• Buserelin.
• Nafarelin.
• Leuprolide.
GH receptor antagonist :
Pegvisomant.
Use : Treatment of Resistant Acromegaly.
Hyperthyroidism :
Hypothyroidsim :
Autacoids 00:00:15
Antihistamines:
First generation Second generation
HCross
1
blockers
BBB: (Sedative). Do not cross BBB (Non sedative).
C/I : Elderly, children, drivers & pilots.
Uses :
• Non allergic rhinitis.
• Used as anti muscarinic in :
a. Extra pyramidal symptoms Uses :
b. Motion sickness • DOC for urticaria.
c. Meniere’s disease. • Rx of allergic rhinitis (DOC is
Note : Max muscarinic block seen with Intranasal steroids : Fluticasone).
1. Promethazine
2. Diphenhydramine
3. Dimenhydrinate
Important drugs : Important drugs :
2. Aspirin :
• Different doses have different effects :
Dose Action
Low dose
Antiaggregant
(50-325 mg OD)
Moderate dose
Antipyretic & analgesic
(325-650 mg SOS)
High dose
Anti inflammatory
(3-4g/d, divided doses)
Chronic gout :
New case of chronic gout
Start Allopurinol
No response
Expectorants :
Guaifenesin : Cause oscillatory movement of the bronchi leading to expulsion of
products.
Mucolytics :
N-acetyl cysteine : Breaks disulfide bonds in the mucus.
Ambroxol/Bromhexine : Depolymerise mucopolysaccharides.
Note :
• PPI’s sholud be consumed 30 mins before food.
• Antacids should be given 30 min after sucralfate.
• Food should be consumed 1 hr before sucralfate.
• Any other drug should be consumed 2hrs before sucralfate.
Prokinetics :
Classification Drugs /side effects
1. Metoclopramide :
• Crosses BBB.
D2 antagonists • Causes EPS.
• Hyperprolactinemia.
2. Domperidone : No EPS.
1. Mosapride
5-HT4 agonists 2. Itopride
3. Prucalopride
1. Erythromycin
Motilin receptor agonists
2. Mitemcinal
CCK1/A receptor agonist 1. Dexloxiglumide
Laxatives :
Increase water in Increase intestinal contrac- Increase stool Softening of
intestine tion bulk stool
Bisacodyl, Senna, Cascara :
1. Osmotic laxatives :
• Promote low grade
Mannitol :
inflammation of large
• Used as second line in Probiotics :
intestine increase Docusate Na+ :
constipation (Costly). Beneficial micro
contraction. They increase
• Used in hepatic en- organisms
• Taken at night. surface tension
cephalopathy as well. • Lactobacillus
• Used for short term treat- of stool
• Saccharomyces
ment of constipation. Collapses stool.
Polyethylene glycol : • B. clausii
• Senna causes melanosis
DOC for IBS associated
coli and pink/yellow brown
constipation.
discoloration of urine.
Hematology 00:47:03
Antiaggregants :
Drugs Uses Side effects
COX-1 inhibitor : Primary prophylaxis of
Bleeding
Aspirin : TXA2 synthesis MI & stroke.
C/I : Cerebrovascular
Primary prophylaxis of
PAR 1 blocker : Vorapaxar disorders (Intracranial
MI.
bleed )
GP IIb/IIIA blockers :
• Abciximab PCI in MI. Bleeding
• Tirofiban Unstable angina. Thrombocytopenia
• Eptifibatide
Irreversible Reversible
1. Clopidogrel : Primary prophylaxis of 1. Cangrelor :
MI and stroke. • Adenosine analog : IV & short act-
2. Ticlopidine : ing.
S/E : Agranulocytosis, TTP-HUS, • Use : PCI in MI.
thrombocytopenia. 2. Ticagrelor :
3. Prasugrel : • Oral
• Causes intracranial bleed. • Use : Acute coronary syndrome,
• C/I in stroke/TIA. prophylaxis of MI and stroke.
• Use : PCI in MI.
Anticoagulants :
Drugs Uses Comments
Direct acting oral No monitoring required.
• DVT Rx.
anticoagulant (DAOC) : Incase of bleeding (D/t
• DOC DVT prophylaxis.
• Oral DTI : Dabigatran overdose) :
• DOC prophylaxis of
• Oral Xa inhibitors : • Dabigatran :
thrombosis in non val-
4. Apixaban Idarucizumab
vular atrial fibrillation
5. Rivaroxaban • Oral Xa inhibitors :
(Native valve).
6. Edoxaban Andexanet alfa
• Skin necrosis : Due to
rapid in proteins C and
S.
• DVT Rx & prophylaxis. • Purple toe syndrome :
Warfarin :
• DOC for prophylaxis of Cholesterol embolus.
• Blocks VKOR .
thrombosis in • Teratogenic : Mid facial
• Decreases levels of
valvular atrial hypoplasia, stippled epi-
factors II,VII,IX,X &
fibrillation physeal calcification, CNS
proteins C and S.
(Mechanical valve). defects.
Antidote : Vitamin K &
4 factor prothrombin com-
plex > FFP
Warfarin DOAC
S/E of heparin :
• H : Hyperkalemia, Hair loss.
• O : Osteoporosis.
• T : Thrombocytopenia.
Fibrinolytics :
t-PA
Plasminogen Plasmin Breaks fibrin
t-PA analogs :
1. Alteplase
2. Reteplase
3. Tenecteplase (Most clot specific).
Given in IV form.
Use : STEMI
S/E : Bleeding (DOC for bleeding : Tranexemic acid > Epsilon aminocaproic acid).