IMPORTANT PHARMACOLOGICAL DEFINATIONS

Pharmacology Study of drugs, drug effect on body and body response to drug.
Drug Any agent which is used for diagnosis (X-ray), prevention
(vaccines), and treatment.
Pharmacodynamics What drug does to the body?
Pharmacokinetics What does body do to the drug?
Antagonism The opposition between 2 or more medications.
E.g. narcotics and Naloxone

Hypersensitivity A reaction to a drug that is more profound than expected and

which often result in an exaggerated immune response
Idiosyncrasy A reaction to a drug that is significantly different from what is
expected
Potentiation Enhancement of a drug’s effect by another drug
E.g. Promethazine may enhance the effect of morphine
Synergism The combined action of 2 or more drugs that is greater than
the sum of the 2 drugs action independently
Therapeutic Index The difference between the therapeutic threshold and the
amount of the drug considered to be toxic (safe and effective
range)
Tolerance The decreased sensitivity or response to a drug that occurs
after repeated doses.
Tachyphylaxis Rapid development of tolerance
Orphan Drug Drug or biological product developed to treat a rare medical
condition.

IMPORTANT POINTS ON PHARMACOKINETICS AND PHARMACODYNAMICS

 Pharmacokinetics is also known as ADME studies

 Passive diffusion is major process for drug absorption. It is explained by Fick’s first law
 Pore transport is also known as convective transport, bulk flow, and filtration. It
depends on the hydrostatic force or osmotic difference between membranes.
 Facilitated diffusion is carrier medicated transport (downhill transport). Driving force is
the concentration gradient. No energy is required.
 Active transport requires energy in the form of ATP.
 Rate limiting step of drug absorption is “Rate of Dissolution”
 Therapeutic index (TI) : Lethal dose/ Effective dose (Remember TILE)
 Symport: Transport of molecules in the same direction
 Anti-port: Movement of molecule in opposite direction.
 Rate limiting step for distribution is “Tissue permeability”
 High protein bound drug are largely restricted to vascular compartment. So they have
low volume of distribution. These types of drug are long acting.
 More than one drug can bind to the same site causing displacement interaction. Eg.
Aspirin displaces sulfonylureas, phenytoin displace warfarin

Drug That Binds To Albumin Drug That Bind To Alfa-1 Glycoprotein

(acidic drugs) (basic drug)
 NSAID’s  Lidocaine
 Phenytoin  Disopyrmide
 Valporic acid  Imipramine
 Warfarin  Propranolol
 Benzodiazepines  Prazosin
 Barbiturates  Quinidine
 Penicillins  Verapamil
 Sulfonamides
 Tolbutamide
 Tetracyclines

 Drug having high volume of distribution ; Chloroquine, Digoxin, Doxepin, Flurazepam,

Haloperidol, Azithromycin, Amiodarone
 Drug undergoing different conjugation reactions
GLUCURONIC ACID ACETYLATION
 Chloramphenicol  Sulfonamide
 Aspirin  Isoniazide
 Paracetamol  PAS
 Diazepam  Dapsone
 Lorazepam  Hydralazine
 Morphine  Clonazepam
 Metronidazole  Procainamide
METHYLATION SULFATE CONJUGATION
 Adrenaline  Chloramphenicol
 Histamine  Methyldopa
 Nicotinic acid  Sex-hormones
 Methyldopa
 Captopril

 Drug having high first pass metabolism : Lidocaine, Isoprenaline, Hydrocortisone,

Testosterone, Propranolol, Salbutamol, Glyceryl Trinitrate, Morphine
 Weak base ionize more and are less reabsorbed in acidic urine
 Weak acid ionizes more and are less reabsorbed in alkaline urine
  Alkalization of urine is done with Na2CO3
 Acidification of urine is done with NH4Cl
 Almost complete elimination of drug occurs in 4-5 half lives
 Creatinine clearance gives a measure of renal function.
 Normal GFR: 120ml/min
 Steady state : Rate of administration = rate of elimination (Achieved after 4-5 half life)
 IMPORTANT HALF LIFE OF SOME DRUG
DRUG HALF-LIFE
Aspirin 4 hrs
Phenobarbitone 90 hrs
Digoxin 40 hrs
Captopril 2 hrs
Penicillin G 30 min
Doxycyclin 20 hrs
Amphetamines 20 hrs
Cloroquine 45-55 days
Amiodarone 58 days

 ZERO ORDER AND FIRST ORDER KINETICS

ZERO ORDER FIRST ORDER

Constant amount of drug is eliminated Constant fraction of drug is eliminated

Independent to drug plasma concentration Directly dependent to drug plasma
concentration
T1/2 depends on plasma concentration T-1/2 remains constant
C=Co – kt C=Co €-kt
T1/2 = 0.5Co / k T1/2= 0.693/k

DRUG AND THEIR ACTIVE METABOLITE

DRUGS ACTIVE METABOLITE

Allopurinol Oxipurinol
Amytryptylline Nortryptylline
Carbamazepine Carbamazepine-10,11-epoxide
Codeine Morphine, Norcodeine
Diazepam Oxazepam
Prednisone Prednisolone
Spironolactone Canrenone

NAME OF THE DRUGS AND SIDE EFFECTS

S.N NAME OF THE DRUG SIDE EFFECTS

1. ACE inhibitors Dry cough
2. Amphotericin-B Nephrotoxicity
Shake and bake syndrome
3. Ampicillin Hypersensitivity
4. Androgen Virilization
5. Anti-psychotics Sedation, Orthostatic hypotension,
Tardive dyskinesia
6. Anti-TB Hepatotoxicity
7. Aspirin Hepatotoxicity,
Reyes syndrome
8. Atropine Dryness of mouth,
Blurred vision,
Constipation

9. Celecoxib, Valdecoxib(selective COX-II Inhibitor ) Hepatotoxicity

10. Chlorambucil Alopecia
11. Chloramphenicol Gray baby syndrome,
Bone marrow depression
12. Chloroquine Phototoxicity
13. Ciprofloxacin Phototoxicity
14. Clofazimine Pigmentation of skin,
Discoloration of urine
15. Clozapine Agranulocytosis
16. Erythromycin Cholestatic Juandice
17. Ethambutol Optic neuritis,
Retrobulbular neuritis
18. Hydrochlorthiazide Hypokalamia
19. Isoniazid Peripheral Neuritis
Hepatotoxicity
20. Metronidazole Disulfiram like reaction
21. Minoxidil Hirsutism
22. Morphine Constipation
23. Nimesulide Hepatotoxicity
24. Nitrogen mustard Bone marrow depression
25. Nitroglycerin Palpitation
26. Penicillin-G Jarisch Heximer Reaction

27. Phenformin Lactic acidosis,

Metformin GI disturbance ,
Metallic taste
28. Phenytoin Hirsutism
Gingival hyperplasia
Phenytoin syndrome
29. Quinidine Cinchonism
30. Quinine sulphate Black water fever
31. Repaglinide Althralgia
32. Rosaglitazone Anemia, weight gain
33. Sitagliptin Coldness
34. Spironolactone Hyperkalamia
Gynacomastia

35. Cemitidine Gynacomastia

Isoniazid
Spironolactone
Digoxin
Estrogen
36. Sulfonyl ureas derivatives Bone marrow depression
37. Terfenadine Type-I arrhythmia
38. Tetracyclines Discoloration of teeth
Fancony syndrome
Phototoxicity
Nephrotoxicity
39. Thalidomide Phocomelia
40. Bleomycin Pulmonary fibrosis
Cyclophosphamide
Amiodarone
41. Doxorubicin Cardiotoxicity
42. Cisplatin Ototoxicity,
Neurotoxicity,
nephrotoxicity
43. Morphine Pin point pupil,
Straubb syndrome
44. Rifampicin Red-orange discoloration of urine
45. Indomethacin Frontal headache
46. Vancomycin Red man syndrome
47. Nicotinic acid Flush
48. Sulfonamide SJS,
Kernicterus,
Uticaria

49. Aminoglycoside Ototoxicity

Neurotoxicity
Nephrotoxicity
50. Chloroquine Cardiotoxicity
Retinopathy
Discoloration of hair
Diarrhea
51. Doxycycline Esophageal ulcer
52. Vincristin Neuropathy
53. Cyclophosphamide Alopecia
Pancretitis
54. Amiodarone Blue baby syndrome
Nausea
Corneal deposit
Intestitial lungs disease
Pulmonary fibrosis
55. Sodium valporate Teratogenic
Valporic acid Curling of hair
56. Carbamazepine Aplastic anemia
57. Statins Hepatotoxicity
Cataract
Rhabdomylosis
Diabetes
58. Lithium Leukocytosis
Diabetes insipidus
Tremor
Hypothyroidism
59. Corticosteroids Crushing syndrome
Osteoporosis
Hirsutism
Obesity
60. SSRI’s Serotonin syndrome
Insomnia
61. Beta blockers Bronchospasm
GI effects
Nightmares
62. Acyclovir Crystal urea
Neurotoxicity
 63. Zidovudine Myleosupression

CAPSULE SIZE AND THEIR APPROXIMATE CAPACITY IN mg and ml

CAPSULE SIZE Mg ML
000(Largest) 950 1.37
00 650 0.95
0 450 0.68
1 300 0.50
2 250 0.37
3 200 0.30
4 150 0.21
5(Smallest) 100 0.13

PROPERTIONS REQUIRED FOR A PRIMARY EMULSION

TYPES OF OIL OIL: WATER : GUM RATIO

Fixed oil 4:2:1
Mineral oil 3:2:1
Volatile oil 2:2:1
Oleoresins 1:2:1

SPANS: SORBITON ESTERS

TWEENS: POLYOXY ETHYLENE SORBITON ESTERS
Spans Tweens
Sorbiton monolaurate 20 (L) Polyoxyethylene sorbiton monolaurate
S. monopalmitate 40 (P) POES monopalmitate
S. monostearate 60 (S) POES monostearate
S. monooleate 80 (O) POES monooleate

SOLUBILITY CHART

DESCRIPTIVE TERM APPROX VOL. OF SOLVENT IN ml/gm of

SOLUTES
Very soluble Less than 1
Freely soluble 1 to 10
Soluble 10 to 30
Sparingly soluble 30 to 100
Slightly soluble 100 to 1000
Very slightly soluble 1000 to 10,000
Practically insoluble More than 10,000

STORAGE TEMPERATURE

Cold temperature 2-8 degree Celsius

Cool temperature 8-25 degree Celsius
Room temperature Prevail ling in the working area
Warm temperature 30-40 degree Celsius
Excessive heat >40 degree
CARR’S INDEX

% Carr’s index = (Tapped density-Bulk density) / Tapped density * 100

HAUSNER’S RATIO

Hausner’s Ratio = Tapped density / Bulk density

% carr’s Index Flow character Hausner Ratio

< or = 10 Excellent 1 - 1.11
11 - 15 Good 1.12 – 1.18
16 - 20 Fair 1.19 – 1.25
21 – 25 Passable 1.26 – 1.34
26 – 31 Poor 1.35 – 1.45
32 – 37 Very poor 1.46 – 1.59
> 38 Very very poor >1.6

ANGLE OF REPOSE

Tan θ = h/r

ANGLE OF REPOSE FLOW CHARACTER

25 – 30 Excellent
31 – 35 Good
36 – 40 Fair
41 – 45 Passable
46 – 55 Poor
56 – 65 Very poor
>65 Very very poor
ANTIDOTES FOR SOME DRUGS

DRUG NAME ANTIDOTE

Acetaminophen N-acetyl cysteine
Alcohols (ethylglycol, methanol) Ethanol
Fomepizol
Heparin Protamine
Warfarin Vitamin K
TCA’s Benzodiazepine
Phenytoin
Physiostigmine
SSRI’s Cycloheptadine
Benzodiazepine Flumazenil
Beta antagonists Glucagon
Epinephrine
Calcium antagonists Glucagon
Insulin
Cyanide Amyl nitrate
Sodium nitrate
Sodium thiosulphate
Digoxin Digibind
Iron Deferoxamine
Isoniazid Pyridoxine (reverse INH induced seizures)
Lead Calcium disodium EDTA
BAL(Dimercaprol)
Opiates Naloxone
Organophosphates Atropine, Pralidoxamine
Theophylline Charcoal
Sulfonylureas Octreotide
Glucose
Arsenic EDTA
Copper Penicillamine
Methemoglobin Methylene blue
Anti-cholinergic Physostigmine

SYNONYMS AND THEIR COMMON NAME

Epsom salt Magnesium sulphate
Calomel Mercurious chloride
Alum Potassium aluminium sulphate
Precipitated chalk Calcium carbonate
Bleaching powder Chlorinated lime
Laughing gas Nitrous oxide
Washing soda Sodium carbonate
Baking soda Sodium bicarbonate
Lugols solution Aqueous iodine solution

VACCINES

LIVE ATTENUATED INACTIVATED RECOMBINANT

Measles Rabies Hepatitis B
Mumps Influenza
Polio Tetanus TOXOID
Rubella Hepatitis A Diphtheria
Typhoid Tetanus
Varicella
Tuberculosis
Yellow fever

TEST ORGANISM FOR MICROBIOLOGICAL ASSAY OF ANTIBIOTICS

Amphotericin B Saccharomyces cerevisiae

Bacitracin Micrococcus luteus
Bleomycin Mycobacterium smegmatis
Kanamycin Bacillus pumilis
Neomycin Staphalococcus epidermis
Rifamycin Bacillus subtilis
Streptomycin Bacillus subtilis
Klebsiella pneumoniae
Tertracycline Bacillus cereus
Staphylococcus aureus

DISEASE ASSOCIATED WITH ALTERED NEUROTRANSMITTERS LEVELS IN BRAIN

DISEASE NEUROTRANSMITTERS LEVEL
Parkinsonism Decreased dopamine in straiatum
Schizophrenia Increased dopamione levels
Depression Decreased Norepinephrine and Serotonin l
Mania Increased NE and 5-HT
Hallucination Increased 5-HT
Alzheimer’s Decreased acetylcholine and destruction of
cholinergic neurons
Athetosis Decreased GABA in putamen
Seizures Increased glutamate level
Decreased GABA level

MICROSOMAL ENZYMES INDUCERS AND INHIBITORS

ENZYME INDUCER ENZYME INHIBITOR

Mnemonics (GPRS Cell Phone) Mnemonics (SICK FACES. COM)
G: Gresiofulvin S : Sodium valporate
P : Phenytoin I : Isoniazide, Itraconazole
R : Rifampicin C : Cemitidine, Clarithromycin
S : Smoking, Sulphonyl ureas K : Ketoconazole
Cell : Carbamazepine, chloral hydrate F : Fluconazole
Phone : Phenobarbitone A : Alcohol, Allopuinol, Amiodarone
C : Ciprofloxacin, CCB(Diltiazem)
E : Erythromycin
S : Sulfonamides
C : Chloramphenicol
O : Omeprazole
M : Metronidazole, Malaria(Quinidine)

DIAGONSTIC TESTS FOR DIFFERENT DISEASE

NAME OF THE DISEASE DIAGNOSTIC TESTS

Syphilis Emzyme immunoassay (EIA) test
Diphtheria Schick test
T.B Mantoux test
Typhoid Widal test
Rheumatoid arthritis Rose water test
Brucellosis COOMBS test(opsonization test)
Scarlet fever Dick test
To detect human chronic gonadotropin in Radio immune assay(RIA)
serum of woman

TESTS AND THEIR USES

TEST IDENTIFY
Carrprice test Vitamin A
Gothlin test Scurvy
Murexide test Uric acid
Biuret test Peptides
Legals test For estimation of acetone
Ames test Carcinogenicity

EASY TO REMEMBER

Morphine side effects: MORPHINE Drug causing Torsades de Pointes: APACHE

 Myosis  Amiodarone
 Out of it(sedation)  Procainamide
 Respiratory depression  Arsenium
 Pneumonia(aspiration)  Cisapride
 Hypotension  Haloperidol
 Infrequency(constipation, urinary  Erythromycin
retention)
 Nausea
 Emesis
Aspirin side effects: ASPIRIN SSRIs side effects: SSRI
 Asthma  Serotonin syndrome
 Salicylism  Stimulate CNS
 Peptic ulcer disease  Reproductive dysfunction in male
 Intestinal blood loss  Insomnia
 Reyes syndrome
 Idiosyncracy
 Noise(tinnitus)
Inhalation anesthetics: SHINE Teratogenic drugs
 Sevoflurane  Warfarin
 Halothane  Thalidomide
 Isoflurane
 Nitrous oxide
 Enflurane
Gynaecomastia causing drugs: DISCOS Anti- rheumatic agents: CHAMP
 Digoxin  Cyclophosphamide
 Isoniazid  Hydroxychloroquine and chloroquine
 Spironolactone  Auranofin and other gold compounds
 Cimetidine  Methotrexate
 Oestrogens  Penicillamine
 Stilboestrol
Phenytoin adverse effect : PHENYTOIN Sodium valporate side effects: VALPORTAE
 P-450 inducer  Vomiting
 Hirsutism  Alopecia
 Enlarged gums(gum hyperplasia)  Liver toxicity
 Nystagmus (not able to control eye  Pancreatitis/ Pancytopenia
movement)  Retention of fats(weight gain)
 Yellow browning of skin  Oedema(peripheral oedema)
 Teratogenicity  Appetite increase
 Osteomalacia  Enzyme inducer
 Interference with B12
metabolism(hence anemia)
 Neuropathies: Vertigo, ataxia,
headache
Amiodarone side effects: 6 P’s Antiparkinson drugs : SALAD
 Prolongs action potential duration  Selegiline(MAO-B inhibitor)
 Photosensitivity  Anti-cholinergics (trihexyphenidyl,
 Pigmentation of skin benzhexol)
 Peripheral neuropathy  L-dopa + peripheral decarboxylase
 Pulmonary alveolitis and fibrosis inhibitor(carbidopa, benserazide)
 Peripheral conversion of T4 to T3 is  Amantadine
inhibited(hypothyrodism)  Dopamine postsynaptic receptor
agonists(bromocriptine, pergolide)
Therapeutic index formula: TILE Adverse effects of tetracyclines-(KAPIL DEV)
TI = LD/ED  Kidney toxicity
 Anti-anabolic effect
 Phototoxicity
 Liver toxicity
 Diabetes insipidus
Captopril side effects(CAPTOPRIL) Lithium side effect: LITH
 Cough angioedema  Leukocytosis
 Agranulocytosis  Insipidus
 Proteinuria/ potassium excess  Tremor/ teratogenesis
 Taste changes  Hypothyroidism
 Orthostatic hypotension
 Pregnancy contraindication/ pressure
drop(first dose hypertension)
 Renal failure
  Indomethacin inhibition
 Leucopenia/ liver toxicity

Myocardial Infarction signs and symptoms; MI basic management: BOOMAR

PULSE  Bed rest
 Persistent chest pains  Oxygen
 Upset stomach  Opiate
 Lightheadedness  Monitor
 Shortness of breath  Anticoagulant
 Excessive sweating  Reduce clot size
Treatment of heart failure: ABCDE
 ACE inhibitors
 Beta-blockers
 Calcium channel blockers
 Diuretics
 Endothelin converting enzyme
inhibitors

BLOOD GROUP AND ITS COLOR OF LABEL

BLOOD GROUP COLOR OF LABEL

O Blue
A Yellow
B Pink
AB white

SPECIFIC ENZYME INHIBITION

NON COMPETITICE INHIBITOR ENZYME

Acetazolamide Carbonic anhydrase
Aspirin, Indomethacin Cyclo-oxygenase
Diuslfiram Aldehyde dehydrogenase
Omeprazole H+K+ ATPase
Digoxin Na+K+ ATPase
Theophylline Phosphodiesterase
Propulthiouracil Peroxidase in thyroid
Atorvastatin HMG-CoA reductase
Sildenafil Phosphodiesterase-5
BETA BLOCKERS

Agents with intrinsic sympathomimetic action Agent with grater aqueous solubility
(ISA)  ATENOLOL
 ACEBUTOLOL  NADOLOL
 PINDOLOL  SOTALOL

Agents with membrane stabilizing effects Agents with anti-oxidant effect

 ACEBUTOLOL  CARVEDILOL
 BETAXOLOL  NEBIVOLOL
 PINDOLOL
 PROPRANOLOL
Agents specifically indicated for cardiac Agents specifically indicated for congestive
arrhythmia heart failure
 ESMOLOL  BISOPROLOL
 SOTALOL  CARVEDILOL
 Sustained-release METOPROLOL
 NEBIVOLOL
Agents specifically indicated for glaucoma Agents specifically indicated for myocardial
 BETAXOLOL infraction
 CARTELOL  ATENOLOL
 LEVOBUNOLOL  METOPROLOL
 TIMOLOL  PROPRANOLOL
Agents specifically indicated for migraine CONTRAINDIATION OF BETA BLOCKER
prophylaxis  Diabetes
 PROPRANOLOL  Asthma
 TIMOLOL  Partial heart block
 Slow heart rate
 COPD
 Electrolyte disbalance(HYPERKALEMIA)

SOME IMPORTANT PH VALUE

BLOOD 7.4
TEAR 7.2
SKIN 7.4
SECRETION OF SKIN 5.5
GASTRIC JIUCE INFANTS:5, ADULTS:2
SALIVA 6.3-6.7
URINE 4.4-8
STOOL APPROX 6
BILE JUICE 8-8.6
SEMEN 7.2-8
VAGINA 3.8-4.5

MECHANISM OF ACTION

DRUG MECHANISM OF ACTION

RIFAMPICIN DNA Dependent RNA Polymerase
ZIDOVUDINE RNA Dependent DNA polymerase
Captopril ACE Inhibitor
Nifedipine, Diltiazem Ca Channel Blocker
Aspirin COX inhibitor
Benzodiazepine GABA facilitator
Barbiturates GABA mimetic
Methotrexate Antimetabolites
Fursemide Loop diuretics
Chloroquine Alteration of bacterial DNA
Amantidine,Acyclovir Inhibition of viral replication
Loratatidine, fexofenadine, cetrizine H1 blocking agent
Ranitidine,cimetidine, Famotidine H2 blocking agent
Omeprazole,Pentoprazole Proton pump inhibitor
INH Mycolic acid synthesis inhibitor
Ibuporofen, oxyphenbutazone Prostaglandin synthesis inhibitor
Beta lactum antibiotic ,Bacitracin, Vancomycin Inhibit cell wall synthesis
Amphotericin-B, Polymixin-B, Nystatin Causes leakage of cell membrane
Trimethoprim, sulfonamide, Inhibit folic acid pathway
Aminoglycoside, nitrofuran, tetracycline Inhibit 30s subunit ribosome
Clindamycin, chloramphenicol, macrolides Inhib 50s subunit of ribosome
Nalidixic acid, quinolones Inhibit DNA-Gyrase and inhibit replication
Ephedrine Release of nor epinephrine
Clotrimazole, miconazole, ketoconazole Ergosterol biosynthesis inhibitors
Physostigmine, neostigmine, edrophonium Acetylcolinesterase inhibitors
Zidovudine Reverse transcriptase inhibitor
Memantine, nitrous oxide NMDA receptor antagonist
Doxorubicin DNA intercalating agent
Phentolamine Alpha receptor antagonist
Norephinephrine Alpha receptor agonist
Isopreterenol, salbutamol Beta receptor agonist
Acetazolamide Carbonic anhydrase inhibitor
Theophylline Phosphodiestrase inhibitor
Heparin Thrombin action prevention
Allopurinol Xanthine oxidase inhibitor
Ketotifen Mast cell stabilizer
Montelukast , Zafirlukast Leucoterine receptor antagonist
SOME IMPORTANT DRUG INTERACTION

Drug Interaction EFFECT

Aluminium Hydroxide Gel + Pseudoephedrine Decrease the effect of drug due to increases
pH of the gastric fluid
Ciprofloxacin + Theophylline Increase pH level of theophylline
Aminoglycoside + Beta-Lactum Antibiotic Synergestic effect but if given in same syringe
it becomes inactivated due to complex
formation
Cortisone + Ampicillin Antagonist
Erythromycin/Clarithromycin + Phenytoin Increase the level of phenytoin
Methotrexate + Sulfamethoxazole Displace from binding site and increase free
plasma concentration of drug
Amphotericin B + Flucytosine Synergestic effect
Ketoconazole + Amphotericin B Antagonized effect due to decreases
ergosterol level
Gresiofulvin + Alcohol Potentiate toxicity if alcohol
Mao Inhibitors + Pethidine Hyperpyrexia
Tca + Ssri’s TCA toxicity
Warfarin + Ciprofloxacin / Clarithromycin/ Increase effect of warfarin
Metronidazole
Warfarin + Nsaid’s Increase risk of bleeding, Increase INR
Fluoroquinolone + Sucralfate Decrease absorption of fluoroquinolone
Phenytoin + Rifampin Decreased phenytoin levels
Ocp + Rifampicin Decrease effectiveness of oral contraception
Sildenafil(Viagra) + Nitrates Dramatic hypotension
Hmg-CoA Reductase + Niacin/ Gemfibrozil / Possible rhabdomyolysis
Itraconazole
Ssri + Tramadol Increase potential for seizures, serotonin
syndrome
Amiodarone + Quinolones Increase risk of TdP and/or QT prolongation in
ECG
Warfarin + Thyroid Hormone Increased bleeding risk
IMPORTANT FACTS
 Lipid insoluble and water insoluble drugs are not absorbed from gut.
 Most of the drugs are weakly acidic are weakly basic because stronger forms has high
ability to form corresponding ions.
 Most (90%) of drugs absorbed through passive diffusion(non-ionic diffusion)
 0% protein binding – Lisinopril
 99% protein binding - oxyphenbutazone (metabolite of phenylbutazone)
 To show an efficient drug action protein binding should be moderate, insufficient
protein binding shows less Vd & high protein binding lessens amount of drug at active
site.
 Extent of binding ----- albumin > acid glycoprotein > lipoprotein > globulins.
 Drug having less Vd means its not bioavailable.(i.e decreased rate & amount of drug)
 Bioavailability of Higher to Lower ------- parenteral > oral > rectal > topical.
 Short acting barbiturates are due its rapid rate of distribution from brain.
 Only unbounded drug (free form) undergoes metabolism.
 The unbound drug 1st reaches liver from where it goes to other parts like kidneys
 Only lipid soluble and non-ionic drugs can enter brain.
 All orally administered drugs undergo first pass metabolism.
 Propanolol & Ca++ channel blockers have extensive first pass metabolism.
 Mainly metabolism occurs to excrete the drug.
 Acidic drugs are exerted at basic pH & vice-versa.
 Absorption, Distribution, Elimination follows 1st order kinetics.
 Drugs showing 0 order elimination kinetics are aspirin, ethanol, phenytoin, Theophyline,
Tolbutamide, phenylbutazone, Warfarin, Heparin, salicylates etc.
 Metabolism, Protein binding, carrier mediated transport at saturated conditions, IV
infusion IM implants, osmotic pumps undergo 0 order kinetics i.e. rate or process
directly proportional to concentration or amount of reactants.
DRUG OF CHOCIE

CONDITION DRUG
Paracetamol poisoining Acetyl cysteine
Acute bronchial asthma Salbutamol
Acute gout NSAID’s
Acute hyperkalemia Calcium gluconate
Digitalis toxicity Digibind
Acute migraine Sumatriptan
Cheese reaction Phentolamine
Atropine poisoning Physostigmine
Cyanide poisoning Amyl nitrate
BDZ poisoning Flumazenil
Cholera Tetracycline
KALA AZAR Liposomal Amphotericin-B
Iron poisoning Desferrioxamine
Methicillin resistance Streptococcus aureus Vancomycin
(MRSA)
Vancomycin resistance Streptococcus aureus Linezolid
(VRSA)
Acute hyperkalemia Ca. GLUCONATE
GERD PPI
Chemotherapy induced vomiting 5HT3 antagonist
Vit. K Poisoning Protamine sulphate
COPD Anticholinergic(Tiotropium)
Warfarine overdose Vitamin-K
OCD Fluoxetine
Alcohol poisoning Fomepizole
Anaphylactic shock Adrenaline
Casodilatory shock Nor-Adrenaline
Cardiogenic shock Dobutamine
PSVT 1st. Adenosine 2nd. Verapamil 3rd. Digoxin
Ectopic pregnancy Methotrexate
Induction of labour Oxytocin
Hypertension in pregnancy Methyldopa
Seizure in eclampsia MgSO4
Hypertensive emergency in pregnancy Labetalol
Gonorrhea Ceftriaxone
Pregnancy mania Olanzapine
Hypothyroidism in children Thyroxine
Hyperprolactinemia Bromocriptine, Cabergoline
Chronic gout Allopurinol
Thyroid storm Propylthiouracil
Deep vein thrombosis Low mol. Weight heparin
Typhoid fever in pregnancy Ceftriaxone
Mania Lithium
Myasthenia gravis Neostigmine
Prevention of neural tube defect Folic acid
Anxiety BDZ
Amoebiasis Metronidazole
Conn syndrome Spironolactone
Thiazide induced hypokalemia Spironolactone
Enuresis Imipramine
Wooping cough or Pertusis Erythromycin
Malaria in pregnancy Chloroquine
Allergic contact dermatitis Steroids
ZE Syndrome PPI
Chancroid Cotrimoxazole
Trigeminal neuralgia Carbamazepine
Opoid withdrawl Methadone
Alcohol withdrawal Chlordiazepoxide, Diazepam
Lithium induced neuropathy Amloride
Filariasis Diethylcarbamazine citrate
Chicken pox Acyclovir
Leprosy Dapsone, Rifampicin
Tuberculosis R.I.P.E.S
Syphilis Penicillin

DISTINCT DEFICIENCY CONDITIONS OF CERTAIN B-COMPLEX VITAMINS ARE KNOWN

VITAMIN DEFICIENCY
Thiamine (B1) Beriberi
Niacin(B3) Pellagra
Riboflavin Cheilosis, Glossitis
Pyridoxine(B6) Peripheral neuropathy
Folic acid(B9) Macrocytic anemia
Cobalamine(B12) Pernicious anemia

 A combination therapy of vitamin B12 and folic acid is commonly employed to treat the
patients of megaloblastic anemia
 Megadoses of niacin are useful in the treatment of hyperlipidemia
 Long term use of isoniazid for the treatment of tuberculosis causes B6 deficiency
  Folic acid supplementation reduces elevated plasma homocysteine level which is
associated with atherosclerosis and thrombosis.
 Sulfonamides serve as antibacterial drugs by inhibiting the incorporation of PABA to
produce folic acid.
 Lipoic acid is therapeutically useful as an antioxidant to prevent stroke and MI

CLASSIFICATION OF ANTI-MICROBIAL AGENTS: On the basis of their mechanism of action

Mechanism of action Drugs

Inhibit bacterial cell wall synthesis Beta lactum
Bacitracin
Vancomycin
Affect the function of cytoplasmic membranes Amphotericin B
Polymyxin –B
Nystain
Agents that inhibit folic acid synthesis Sulfonamides
PAS
Trimethoprim
Agents that inhibit 30S ribosome Aminoglycoside
Nitrofurantoin
Tetracycline
Agents that inhibit 50S ribosome Lincosamide
Chloramphenicol
Macolides
Agents that interfere with nucleotide synthesis Zidovudine
Acyclovir
Flucytosine
Agents that interfere with DNA replication Metronidazile
Quinolones(Inhibit DNA gyrase)
Agents that inhibit DNA Dependent RNA Rifampicin
polymerase

VARIOUS TOXICITY CAUSED BY ANTIBIOTICS

Toxicity Antibiotics
Ototoxicity Aminoglycoside
Vancomycin
Phototoxicity Quinolones
Fluoroquinolones
Hypersensitivity Penicillin
 Cephalosporin
Sulfonamide
Hepatotoxicity Tetracycline
Streptomycin
Isoniazid
Rifampicin

Neurotoxicity Quinolones
Cycloserine
Polymyxin-B
Nephrotoxicity Vancomycin
Polyenes
Polypeptides
Bacitracin
Tetracycline
Aminoglycoside
Alopecia Chlorambucil
Chloramphenicol
Optic neuritis Ethambutol
Peripheral neuritis Isoniazid
Hyperuricemia Pyrazinimide

CLASSIFICATION OF EMULSIFYING AGENTS

Natural agents 1. 0/w

 Acacia
 Tragacanth
 Starch
 Sodium alginate
 Pectin
 Agar
2. W/O
 Bees wax
 Wool fat
 Wool alcohol
Semi-synthetic  Methyl cellulose
 SCMC
 Synthetic  Ammonium carboxymethyl cellulose

CLASSIFICATION OF SURFACTANT

Anionic  Alkali metals , ammonium salts

Cationic  Cetrimide
 Quaternary ammonium compound
Non –ionic  Macrogals (Polyethylene glycol
esters)
 Tweens (Sorbiton esters)
 Spans (Polyoxyethylene sorbitan
esters)

HLB SCALE

0-3 Anti-foaming agents

3-6 W/0 Emulsifying agents
7-9 Wetting and Spreading agents
8-16 O/W Emulsifying agents
13-15 Detergents
15-18 Solubilizing agents

Rheological behavior of liquids

Newtonian liquids Water

Glycerine
Chloroform
Syrup
Very dilute colloidal solution
Non-Newtonian liquids
Plastic flow/ Bringham bodies Flocculated particles in concentrated
suspension
Pseudoplastic flow (Shear thinning material) Synthetic and natural gums
Tragacanth
MC
SCMC
Liquid paraffin
Dilatent flow (Shear thickining material) Suspension containing high concentrated solid
Deflocculated suspension
Starch in water
  Viscosity (dynes/cm) or poise
 Viscosity of gas increase with increase in temp
 Viscosity of liquid decreases with increase in temp

SINGLE POINT MULTIPOINT

 OSTWALD VISCOMETER  Cup and bob(Rotational)
 FALLING SPHERE VISCOMETER  Cone and plate
(Newtonian fluid) (Both Newtonian and non-Newtonian fluid)

 Rate of sedimentation rate is given by stokes law

 Ph : Henderson-Hassel baltch equation
 As temp increase surface tension of a fluid decreases

Coating equipment of tablet

1. Conventional pan system

2. Perforated pan
3. Fluidized bed dryer
4. Spray application system

MATERIAL USED FOR SUGAR COATING

Seal Coating Shellac, Zein

Subcoating Gelatin, Acacia
Smoothing/ Syrup coating Diluents colorant ,cane sugar
Polishing Beewax, Carnuba wax

FLIM COATING

 Tablet, Capsules, Pellets

 Surround them with thin layer of polymeric material
 Film polymers
  Hydroxypropyl methyl cellulose
 Methyl hydroxyethyl cellulose
 Ethycellulose
 Hydroxypropyl cellulose
 Povidone
 Sodium carboxymethyl cellulose(SCMC)
 Polyethylene glycol
 Acrylate polymers

ENTERIC COATING

 To protect the tablet core from disintegration in the acidic environment of the stomach
by employing the pH sensitive polymer.
 Examples
 Cellulose acetate Phthalate(CAP)
 Acrylate polymers
 Hydroxymethylcellulose Phthalate(HMCP)
 Polyvinyl Acetate Phthalate(PVAP)

TABLETS MANUFACTURING DEFECTS

CAPPING AND LAMINATION Capping is partial or complete Due to air trapping

separation of top or bottom Incorrect setup of the press
crown Deep concave punch
Lamination is separation into
two or more distinct layer
PICKING AND STICKING Picking is removal of tablet Engraving or embossing
surface from the punch punches
Sticking refers to tablet
adhering to the dye wall Larger engraving punch
Larger tablet size
MOTTLING Unequal distribution of color Color variation
on a tablet.
Weight variation In-process control measure.

Hardness variation
Double impression Making of new or alternative
print
Uniformity of weight of tablets

Average weight of tablet Percentage deviation

< 80 mg 10
80mg – 250mg 7.5
> 250 mg 5

Disintegration test for tablets (TOTAL 18 TABS USED)

Types of tablets Time

Uncoated 15 min
Film coated 30 min
Sugar coated 60 min
Enteric coated 2 hrs in HCl / 1 hr in buffer
Dispersible 3 mins
Effervescent tablet 3 mins
Sublingual tablet 3 mins

Dissolution test

 Total of 24 tablets are used

According to IP According to USP
TYPE-I : Paddle TYPE-I : Basket
TYPE-II : Basket TYPE-II : Paddle

TABLET EXCIPIENTS

DIULENTS (to increase bulk volume/fillers) Lactose

Sucrose
Dextrose
Starch
Sta Rx 1500
Microcrystalline cellulose
DISINTEGRATING AGENT Starch (maize, corn, potato starch)
Cellulose and its derivatives (MCC,SCMC)
Clays
 SUPER-DISINTEGRANTS
1. SODIUM STARCH GLYCOLATE
2. CROSSCARAMELOSE
3. CROSSPOVIDONE
BINDER AND ADHESIVE Starch paste
Gelatin
Gum acacia,tragacanth
Liquid glucose
Cellulose derivatives
PVP, PEG
LUBRICANT Talc
Magnesium stearate
PEG
GLIDANT Talc
Colloidal silica
Corn starch
Aerosil
ADSORBING AGENT (for eutectic mixture) Mg stearate
Stearic acid
GRANULATING AGENT Starch paste
Acacia,tragacanth
Isopropyl alcohol

IMPORTANT POINTS

 Unequal distribution of color : Mottling

 Excessive moisture in tablet causes sticking
 Anhydrous lactose advantage over hydrous lactose: Absence of millard rxn
 Polyvinyl pyrrilidone is synthetic adhesive
 PEG is water soluble lubricant
 Aerosol is glidant
 Saccharin is 500 times sweeter than sucrose, but carcinogenic and has bitter test
 Enteric coating material : CAP, HPMCP,PVAP
 Causes of tablet defects
Chipping Excessive coating process
Cracking Higher internal stress
Orange peel Poor spreading
Blistering Over heating during spraying
 Dissolution studies : Noyes whitney equation
  Diffusion across membrane : Fick’s law
 PH : Henderson-hasselbatch equation
 Plasticizers provide flexibility examples : Glycerin, sorbitol, castor oil
 Crown thickness of tablet is measured using Sliding caliper scale, micrometer

Types of gelatin

TYPE-A TYPE-B
 Obtained from acid hydrolysis of pork  Obtained from alkaline hydrolysis of
skin bones
 Isoelectric pH : 9  Green bone
 Isoelectric pH : 4.7

Steps involved in making empty gelatin capsules

DIPPINGSPINNINGDRYINGSTRIPPINGTRIMMING AND JOININGPOLISHING

Uniformity of weight of Capsule

Average weight of capsule Percentage deviation

Less than 300 mg 10
300 mg or more 7.5

Disintegration and dissolution

Types of capsule Disintegration time

Hard gelatin capsule 30 mins
Soft gelatin capsule 60 mins

Important points on Capsules

  Plasticizers are used to provide flexibility. Amount of plasticizers is higher in soft gelatin
capsule
 Commonly used plasticizers: Sorbitol,glycerol, propylene glycol
 Opacifiers are added to make capsule shiny : Titanium dioxide
 Bloom strength/ gel strength ofgelatin is 150-250 gm
 Ratio of plasticizer used : 0.3-1.8%
 Rotasort : separate unfilled capsule
 Rotafil : used to fill pellets in capsule
 Quali-seal : used to fill liquid in capsule
 Viscosity of gelatin : 25-45 millipoise
 Capsule are sealed hermetically at 37-40 degree Celsius

Microencapsulation

 Applying thin coating to small particles of solid or droplets of liquids and

dispersion of size upto 5000 micron
 Applications
 Taste masking
 Stabilization to oxidation
 Reduction of volatility
 Reduce gastric irritation
 Sustained release medication
 Microencapsulation process includes Air suspension,coacervation phase
separation, multiorifice-centrifugal process
 Coating material
 Water soluble : Gelatin, Gum Arabica, Starch, PVP, CMC, HEC
 Water insoluble : EC, Polyethylene, polyamide, cellulose nitrate
 Waxes and lipids : Paraffin wax, carnauba wax, spermaceti, beeswax,
stearates
 Enteric coating material : Shellac, CAP, Zein

PARENTERALS

Classification

1. Small volume parenteral

2. Large volume parenteral
Formulation of parenterals

1. Vehicle

Aqueous vehicle Non-aqueous vehicle

 WFI(PH 5.0-7.0)  Peanut oil
Particle not exceeding 10 parts  Corn oil
per million  Cottonseed oil
 SWFI  Sesame oil
 Soyabean oil

2. Preservative

Preservatives Usual concentration (%w/v)

Benzalkonium chloride 0.01
Benzethonium chloride 0.01
Benzyl alcohol 2.0
Phenol 0.5

3. Buffers
- Added to maintain ph
- To stablilize a solution from chemical degradation
- E.g. Citrate buffer, Phosphate buffer, sodium benzoate and benzoic acid
4. Antioxidant
i. To protect formulation from oxidation

Reducing agent Blocking agent

1. Ascorbic acid 1. Tocopherol
2. Sodium bisulphate
3. Sodium metabisulphite
4. Thiourea

5. Tonicity agents
i. Need isotonic solution to avoid destruction of RBC, irritation, tissue
damage(more important for large volume parenterals, rapidly
administered and extravascular injections)
ii. E.g : NaCl, KCl, Dextrose, Mannitol, Sorbitol
6. Suspending agents
i. E.g CMC, Methyl cellulose, gelatin, sorbitol

7. Emulsifying agents
i. Lecithin
ii. Polysorbate 80

QUALITY CONTROL TEST FOR PARENTERALS

 Content uniformity test

 Leaker test
 Pyrogen test
 Sterility test
 1. Membrane filtration method
2. Direct inoculation method (with medias like Fluid Thioglycolate, Soyabean-Casein
Digest Medium)
 Particulate test

Important points on parenterals

 Glass is mainly used as the packaging material for parenterals

TYPE-I Borosilicate glass

TYPE-II Treated soda lime glass
TYPE-III Soda lime glass
 Type-I and type-III glass undergo powder glass test
 Type-II glass undergo water attack test
 Powder glass test measures the leaching property of the internal surface of glass
 Water attack test challenges only the intact surface of the container
 test for rubber
1. sterilization test
2. test for extractable matter
3. fragmentation test
4. test for sulphur, heavy metal, Reducing substance
 Preservative is not used in large volume parenterals
 Disposable syringe is made up of polypropylene
 Permitted limit of solid content in WFI is 10 ppm
 Aqueous injection is sterilized by moist heat sterilization
 Oily injection is sterilized by dry heat sterilization
 Cool place : 8-25 degree Celsius
 Cold place : 2-8 degree Celsius
 Vaccines are kept maintaining the cold chain temperature(2-8)
 Co-solvent is used to increase the solubility. It includes Dimethyl acetamide, Ethanol,
Poly ethylene Glycol
 Local anesthesia used in pareneterals : Procaine HCL, Benzyl alcohol
 Synersis : Shrinkage of gel by extrusion of liquid
 Pyrogen are lipopolysaccharides produced by cell wall of gram (-ve) bacteria

SUSPENSION
Formulation of suspension

Suspending agents 1. Sodium alginate

They form a film around particle and decrease 2. Methylcellulose
interparticle attraction 3. Hydroxyethyl cellulose
They also imparts ciscosity to the solution 4. Hydroxyl propyl cellulose
Wetting agents 1. Tweens
Hydrophilic materials are easily wetted by 2. Span
water while hydrophobic materials are not. 3. Acacia
However, hydrophobic materials are easily 4. Tragacanth
wetted by non-polar liquids 5. Ethanol, glycerol, glycols

Surfactants 1. Polysorbate 80(must widely used)

They decrease the interfacial tension between
drug particles and liquid thus liquid is
penetrated in the pores of the drug particle
and ensure wetiing.
Solvents 1. Alcohol
2. Glycerin
 3. Polyethylene glycol
4. Prlypropylene glycol
Buffers 1. Carbonates
They resist PH change when an acid or base is 2. Citrates
added 3. Gluconates
4. Phosphate

Preservatives 1. Propylene glucol

2. Disodium EDTA
3. Benzalkonium chloride
4. Benzoic acid
Humectants 1. Propylene glycol
They absorbs moisture and vprecent 2. Glycerol
degradation of API by moisture
Anti-oxidants 1. Ascorbic acid
2. Thio glycerol
3. Tocopherols

Important points in suspension

 Particle size
Solution < colloids < suspension
 Coarse and colloidal dispersion system scatter light which is known as tyndall effect
 Rheological evaluation is used to compare different suspensions.
 For an ideal suspension sedimentation volume is equal to one.
 Viscosity of suspension is measured by Brookfield viscometer
 Flocculated suspension has clear supernatant liquid
 Deflocculated suspension has turbid supernatant liquid
 Coarse suspension has particle ranging from size 1-100 micrometer
 Suspension is a heterogeneous mixture
 Sedimentation rate of a suspension is given by Stoke’s Law

EMULSION

Identification test for emulsion

1. Cobalt chloride test

 2. Conductivity test
3. Dilution test
4. Dye test
5. Filter paper test
6. Fluorescent test.
7. Direction of creaming: according to density. w/o emulsion (creaming is downward), o/w
emulsion (creaming is upward)

Instability of emulsion

1. Flocculation
2. Creaming
3. Coalescence
4. Phase inversion

Method of preparation

1. Continental or dry gum method

2. English or wet gum method
3. Bottle or forbes bottle method

Important points to remember in emulsion

 Particle size of emulsion range from 0.1-100 micrometer

 Microemulsion has particle size less than 0.1 micrometer
 Upward creaming is observed in O/W emulsion
 Downward creaming is observed in W/O emulsion
 Flocculation- coalescence –creaming-cracking/breaking
 PROPERTIONS REQUIRED FOR A PRIMARY EMULSION

TYPES OF OIL OIL: WATER : GUM RATIO

Fixed oil 4:2:1
Mineral oil 3:2:1
Volatile oil 2:2:1
Oleoresins 1:2:1