GENERAL PHARMACOLOGY

• Father of Pharmacology – Rudolf Buchhiem• Father of Medicine – Hippocrates• Father of Polypharmacy – Galen• Father of American Pharmacology- John Jacob Abel• Nitrogenous active principle – Alkaloid• Glycosides contain sugar and non sugar part• Non biodegradable implant is – Sialistic• Drug transport Diffusion, Filtration Specialised transport Active transport, facilitated diffusion,Pinocytosis

• BIOTRANSFORMATION- Phase I :- Oxidation, Reduction, Hydrolysis Phase II:-Conjugation (Glucuronide,Sulphate,Acetate)

Glucuronide Conjugation is absent in “Cats”Sulphate Conjugation is absent in “Pigs”Acetylation is absent in “Dogs”

• EXCRETION :- Glomerular filtration, Tubular secretion(Penicillin, Probenicid) Tubular reabsorption

DRUG ACTIONSPECIFIC ACTION:- Receptors, Ion channels, Enzymes, carrier moleculesNON SPECIFIC ACTION:- Physical action : Bulk laxatives, Saline purgatives, Osmotic diuretics, Activated charcoal

DRUG- RECEPTOR INTERACTIONAGONISTS :- Full agonists (eg:- Morphine) Partial agonist Mixed agonists(eg:-Nallorphine) Inverse agonists(eg:- DMCM)ANTAGONISTS:- Naloxone, Yohimbine

Therapeutic index = LD50 ED 50

Therapeutic Ratio = LD25 ED 75Standard safety margin = LD1 ED 99

DRUG INTERACTIONSAdditive Effect : 1+1 = 2Potentiative effect : 1+0 > 1Synergism :1+1 > 2Antagonism : 1+1 < 2

Chemical Antagonism :- BAL + Metal ions (As,Hg) Pb+ Dimercaprol Heparin+ Protamine sulphate

• Functional Antagonism:- Acetyl choline+ Adrenaline• Receptor Antagonism :- Competitive:- Morphine+ Naloxone Non competitive (Irriversible):- Op compoundsFactors affecting1. ROUTE OF ADMINISTRATION MgSO4 :- Orally (Purgative), Externally(Osmotic),

i/v(CNS depression)2.SPECIES Atropine is non toxic to rabbit because of the enzyme

“Atropinase”3.BREED :- Greyhounds are more susceptible to thiobarbiturates.4. Sex:- Male mice more susceptible to nephrotoxic effect of

chloroform. Females are more susceptible to adverse drug effects.

• AGE:- Very young and very old animals are more susceptible

• PREGNANCY:- Oral anticoagulants are more toxic to pregnant animals

• LACTATION:-Enhances the excretion of lipophilic drugs• GENETIC STATUS :- Low level pseudocholinesterase show

prolonged muscular relaxation and apnoea with Suxamethonium .

• NUTRITIONAL STATUS :- Paracetamol more hepatotoxic in animals with protein deficiency

• Tachyphylaxis:- Rapid development of tolerance due to repeated administration of drugs(eg Ephedrine, Tyramine)

ADVERSE DRUG REACTIONS1. Exaggerated effect:- Haemorrhage occurs due to over dosage

of Anticoagulants2. Side effect:- Antihistaminics produce drowsiness3. Secondary effects:- Corticosteroids Suppress defense

mechanism4. Intolerance:-Exaggerated pharmacologic effects5. Hypersensitivity reactions:- Beta lactam antibiotics 6. Idiosyncrasy:-Genetic defect.(Halothane anaesthesia in pigs)7. Photosensitization:- Lantana, Phenothiazine 8. Carcinogenicity9. Mutagenicity10. Teratogenicity

AUTONOMIC NERVOUS SYSTEM• Cholinergic receptors for Acetyl choline are of 2 type Nicotine- Nm, Nn Muscarinic –m1,m2,m3,m4,m5Adrenergic receptors for Nor epinephrine Alpha- α 1, α 2Order:- Norepinephrine (α )>Epinephrine(α β )>Isoproterenol(β) Beta-β1, β2, β3Sympathomimetic amines:- Exogenous catecholamines:- Isoproterenol,Ephedrine. Endogenous catecholamines:- Epinephrine,Nor epinephrine, Dopamine

• Inactivation Of Sympathomimetic amines Tissue uptake mechanism:- Uptake1:-Back to presynaptic nerve terminal Uptake2:-Into effector tissue ,metabolised by MAO and COMTPHARMACOLOGIC AL EFFECTS α 1 :- Stimulation α 2 :- Depression β1 :- Stimulation β2 :- DialatationDopamine receptorsD1:-Vasodilatation of renal and mesenteric blood vesselsD2:-Decreases BP,Vasodialationβ1 :- Positive enotropic effectα 1 :-Vaso constriction

• USES OF EPINEPHRINEReduces bronchospasmTreat hypersensitivity and anaphylaxisProlong local anaesthetic effectsControl local haemorrhageNor epinephrine To correct hypertention induced by spinal anaesthesia

• USES OF DOPAMINE Cardiogenic shockSeptic shockAcute heart failure

• Direct acting drugsEpinephrineNor epinephrinePhenyl ephrineIsoproterenolMetaproterenolTerbutalin

Non catecholaminesPhenyl ephrine,Dobutamine,Ephedrine,Phenyl

propanolamine,Amphetamine

• Adrenergic AntagonistsNon selective-(1)Haloalkylamine/Alkylating agents Eg:-Phenoxybenzamines (2)Imidazole derivatives Eg:-Tolazoline,Phentolamine (3)Ergot Derivatives Eg:- Ergotamines,Dihydroergotamines (4) Miscellaneous (5)Neuroleptics:-Chlorpromazines,Haloperidol (6)Benzodiozoxans:- Dibozane (7)Dibenzazepine Derivatives:- Azapetine

Selective α Adrenergic Antagonists

Selective α1 – Prazosin,Indoramine Selective α2-Yohimbine,Atipamizole

Non Selective β Adrenergic Antagonists Propanalol,Nodolol,Pindolol,Timolol

Selective β Adrenergic Antagonists β1- Metoprolol,Atenolol,Esmolol β2-Butoxamine

Both α ,β Adrenergic Antagonists eg:-Labetolol

• ADRENERGIC NEURON ACTING DRUGS

α methyl β Tyrosine – Metysosin- Depletion of CatecholaminesCarbidopa- Inhibit Dopa Decarboxylase –Parkinson’s disase along

with L- Dopa

α methyl Dopa Form Methyl noradrenaline- False neurotransmitter-Agonist of α2 receptor-Decreases sympathetic outflow

“ Rserpine “(Rauwolfia serpentina alkaloid) – Depletion of Catecholamines

“Bretylium” –Antihypertensive,antiarrhythmic

CHOLINERGIC AGONISTS

Direct acting agents-(Cholinomimetic Esters) Acetyl choline,Bethenecol,Carbachol,Methacholine Cholinomimetic alkaloids- Pilocarpine,Arecoline,Muscarine,NicotineIndirect acting cholinomimetics/Choline esterase inhibitors

1.Reversible Choline esterase inhibitors Eg:- Neostigmine,Pyredostigmine,Edrophonium,Physostigmine2.Irriversible inhibitors Eg:-OP

compounds(Malathion,Parathion,Dichlorvos,Ecothiophate)

Muscarinic ActionVascular dialationFall in BPDepress HeartContraction of Non vascular smooth muscles- GI tractIncrease in tone activity of stomach and intestinal secretionConstriction of pupil

Nicotinic ActionSkeletal muscle fasciculation and increased adrenaline

secretion

CHOLINOMIMETIC ALKALOIDS Pilocarpine from Pilocarpus goborandi

P.microphyllus- Treatment of glaucoma- Stimulate muscarinic receptors.

Arecoline-from Areca catechu acts on muscarinic and nicotinic receptors-Anticestodal,Purgative in in horses

Muscarine- from Amanita muscaria acts on muscarinic receptors

Nicotine- Nicotinia tobacum- Nicotinic receptors

Indirect acting agents – Physostigmine,Neostigmine,Edrophonium

Uses :- 1.To reverse the effects of competitive neuromuscular blocking drugs

2. Myasthenia gravis 3.Impaction and Atony- PhysostigmineIrriversible Choline esterase inhibitorsDichlorvos,Parathion,Malathion,Fenthion,Trichlorfen,ecothiophat

e,Sarin,Tabun,Di isopropyl flourophosphateAction-Interact with esteratic site of cholinesterase enzymeSymptoms Muscarinic,Nicotinic,and delayed neuropathyTreatment:- Atropine- AntimuscarinicOximes:- 2PAM,(Pyrimidine 2-

aldoxime,Diacetylmonoxime,Obedoxim

ANTICHOLINERGIC DRUGS

1. Natural alkaloids- Atropine,Hyoscine2. Semisynthetic –Homatropine,Tropicamide,-Mydriatic propantheline,Iprotropium,Hyoscine butylbromide

SELECTIVE MUSCARINIC RECEPTOR BLOCKER

m1-Pirenzepine,telenzepine

ATROPINE – USES

1. Preanaesthetic (Dose- 0.045mg/Kg Body wt)2. Antispasmodic3. Mydriatic4. Antidote to OP poisoningHomatropine- Mydriatic-Antisecretory-antispasmodic-

Diarrhoea-and GI disordersAUTONOMIC GANGLIONIC STIMULATORY DRUGSNicotinic stimulants:-Natural alkaloids:- Nicotine,LobelineSynthetic :-Tetraethyl ammonium,Dimethyl phenyl piperazoniumMuscarinic stimulants:-Acetyl choline,Muscarine,Methacholine

AUTONOMIC GANGLIONIC BLOCKING AGENTSNicotine,Lobeline,Hexamethonium,Pentolinium,Pentamethoxim,

Mecamylamine,Pompedine,Trimetaphan

SKELETAL MUSCLE REALAXANTS NM BLOCKING DRUGS1.Non depolarising/Competitive D-Tubocurarine,Pancuronium,Gallamine,Dexacurium, Vecuronium,Atracurium,Mivacurium2.Depolarising/Non competitive Suxamethonium,Decamethonium3.Direct acting:- Dandrolene,Quinine

• 4.Centrally Acting:-Methocarbamol,Carisopradol,Guaphenesin,Mephenesin,Diazepam,Chlordiazepoxide,Nuprobamate

• GABA derivative- Baclofen

AUTACOIDSHistamine-Storage-Mast cell poolNon Mast cell poolsINACTIVATION Histamine Histamine N methyl transferase

N methyl Histamine MAO N methyl Imidazole acetic acid Deamine oxidase

Imidazole acetic acid

• Receptors-H1,H2,H3H1Receptors:- Contraction of bronchi and intestine .Increases

capillary permeability and pruritusH2Receptors:- Gastric glands,uterus,Blood vessels,CNSH3Receptors:- Presynaptic neurons of brain modulate(Inhibit)

histamine release- “Triple response”HISTAMINE ANTAGONISTSFirst generation compounds (produce drowsiness)1.Ethanolamines-

Diphenhydramine,Dimenhydrinate,Carbenoxamine,Clemastine fumarate

2.Ethylene diamines:- Mepyramines,Tripelennamine,Antazoline,Methapyriline.

3.Alkyl amine:- Chlorpheneramine,Pheneramine.4.Piperazines:-

Hydroxyzine,Meclizine,Chlorcyclizine,Buclizine,Cennarizine5.Phenothiazenes:-Promethazines,Trimeprazine6.Miscellaneous:- Cyproheptadine,PhenindamineSECOND GENERATION COMPOUNDS1.Piperidines:- Terfenadine,Astemizole,Loratidine,Fexofenadine2.Piperazines:-Ceterizine3.Miscellaneous :- Azelastine,AcrivastineUESES a) Symptomatic treatment of allergyb) Diphenhydramine,Cyclizine is useful in controlled prevention

of motion sickness c) CNS depressant and antimuscarinic activities

SEROTONINSynthesised from tryptophan –In enterochromaffin cells of GI tract-

Degraded by Oxidative deamination by MAO to form 5 Hydroxy Indole Acetic acid

It functions as a precursor of melatonin.Receptors :- 5HT1 to 5H7Intravenous injection:- “Triphasic response”-Early fall ,brief rise ,prolonged

fall in BP.• Selective Agonists• 5HT1A receptor – Buspirone

• 5HT1D- Sumatriptan• 5HT4- Cisapride• Metoclopramide – Non selective-dopamine as well as 5HT receptor• LSD –Synthetic ergot derivative,and potent Nonselective• SELECTIVE 5HT RECEPTOR ANTAGONISTS • Ketanserine,Retanserine,Clozapine,Risperidone,Ondansetron(Nausea

and vomiting)

• NON SELECTIVE ANTAGONISTS Ergot alkaloids, Phenothiazines ,cyproheptadines• KININS Powerful algesic substances:-• Bradykinins,Kallidin,no therapeutic value• Inhibitor of kinin synthesis :- Atropine• 2 types receptors – B1 and B2• ANGIOTENSINS• AT1 and AT2 receptors• Renin secretion inhibitors:- Propanolol• ACE inhibitors Captopril,Enalapril,Quinapril,Ramipril

• ANGIOTENSIN RECEPTOR ANTAGONISTS Losartan,Telmisartan EICOSANOIDES• Prostaglandin E analogoues- Dinoprostone(E2) Mesoprostol(E1)• Cytoprotective and antiulcer effect• Prostaglandin F and Anologues (Dinoprost)-Luteolytic agent-

Synchronisation of oestrous-termination of pregnancy.• Cloprostenol – Synthetic analogue of PGf2α • Induction of oestrous• Induction of parturition• Termination of pregnancy• Inhibitors of Eicosanoisd synthesis – Glucocorticoides, NDIADS

• RUMENOTORICS• 1.Cholinergic agonists- Neostigmine,Carbachol• 2.Prokinetics:- Metaclopramide• 3.Plant alkaloids- Arecoline,Pilocarpine• 4.Bitters:- Gentian,Nuxvomica• Ruminal acidifying agents:- Acetic acid or vinegar(5%)1-2

L• Ruminal alkylating agent:- Mg(OH)2,MgO,CaCO3,NaHCO3

•

• EXPECTORANTS • Secretory / stimulant expectorant• 1.Reflex acting :- Ipecacunha,Balsam of Tolu,Squill• 2.Direct acting:- Guaicol,Guaiphenesin,Volatile

oils,Terpene hydrates• 3.Mixed acting:- KI,NH4Cl• 4.Mucolytic expectorants:- Bromhexine,Acetyl

cysteine• 5. Diluent expectorant:- Aerosols

• ANTITUSSIVES• Peripherally/Locally acting• 1.Demulscents:- Honey,Syrup,Glycerine,Liquorice• 2.Expectorants:- Bromhexine,Water ,aersol• Centrally acting• 1.Opioid/Narcotic Antitussives• Codiene,Hydrocodiene,Butorphanol,Hydromorphine,Morphine• 2.Non Opioid :- Dextramethorphan• BRONCHODIALATORS• 1.Sympathomimetics(Non selective)• Adrenaline,Ephedrine,Isoproterenol• 2.Selective β2 agonists• Clenbuterol,Salbutamol,Terbutalene.• 3.Anticholinergic:- Atropine,Ipratropium• 4.Methyl Xanthines:- Theophylline,Aminophylline

• ENDOCRINE SYSTEM• Replacement therapy with hormone:- GnRH• Gonadorelin:- GnRH• Buserilin:- GnRH analogue• Bromocryptine:- Dopamine Agonist decreases ACTH secretion• Pergolide:- Dopamine Agonist• Selegiline(Deprenyl)Inhibitor of MAO decreases ACTH secretion• ANTITHYROID DRUGS• 1.Inhibitors of thyroxine secretion:-Methimazole,Carbimazole• 2.Destroy thyroid tissue:- Radioactive Iodine• 3.Inhibit hormone release:-Iodides of Sodium and Potassium• 4.Inhibit iodide trapping:- Thiocyanates and Perchlorates

• CORTICOSTEROIDS• Intracytoplasmic receptors• Short acting:- Hydrocortisone,Cortisone• Intermediate acting :-

Prednisolone,Prednisone,Triamcinolone• Long Acting:-

Dexamethasone,Betamethasone,Flumethasone

• GONADAL HORMONES• OESTROGENS• Steroidal oestrogen(Natural)- Estradiol,Ostrone• Semisynthetic:- Estradiol cypionate, Estradiol

valerate,propionate• Synthetic:- Ethynil oestradiol• Non steroidal :- Diethyl stilbesterol,Hexoesterol,benzestrol• USES:- Misalliance in bitches,Induce lactation• Antioestrogens• Oestrogen receptor Inhibitor:- Clomephene,Tamoxiphen• Oestrogen synthesis Inhibitor:-Aminoglutathemide• Clomephene:- Anovulatory Sterility• Tamoxiphen:- Oestrogen dependant breast cancer

• PROGESTERONE• Natural:-Progesterone• Synthetic:-

Medroxyprogestone,Megestrol,melemgestrol,Proligestone,Flugestone,Norgestomet

• ANTIPROGESTINS• Eg;- Mefipristone• • ANDROGENS• Natural- Testosterone• Synthetic –• Testosterone cypionate,Propionate,decanoate,Phenyl

propionate

• ANABOLIC STEROIDS• Stanzolol,Fluoxymesterone,Ethyloesterol,Nand

rolone,Trenbolone.• INHIBITORS OF ANDROGEN SYNTHESIS• Fenasteride:- to treat benign prostatic

hyperplasia• ANDROGEN RECEPTOR ANTAGONIST• Cyproterone acetate,Flutamide• Female Sex hormone;-

Delmadinone(Antiandrogen)

• INSULIN• Short acting: - regular insulin,semiLente insulin• Inermediate:- Lente insulin,Isophane Insulin• Long acting :- Protamine Zinc Insulin,Ultra lente Insulin

• ORAL HYPOGLYCEMIC DRUGS• First generation-Sulphonyl ureas• Chlorpropamide,Tolbutamide,Tolazamide• Second generation-• Glypizide,Gibenclamide,Gliclazide• Biguanides;- Metformin,Phenformin• Thiazolidone drugs:-• Troglitazone,Euglitazone,Proglitazone• Guar gum- Soluble dietary fibre

• ANTIFUNGAL DRUGS• Classification• 1.Antifungal antibiotics• a) Polyenes-Amphotericin B,Nystatin• b)Heterocyclic benzofurans eg:-Griseofulvin• 2.Antimetabolites eg:- Flucytosine • 3.Azols a)Imidazoles:- Ketoconazole• b) Triazoles:-Fluconazole• 4.Allylamines:- Terbinafine

• Mechanism of action• 1)Amphotericine B;-Affinity for ergosterol of cell

wall of fungi- alters membrane permeability• 2)Griseofulvin:-interfere with polymerisation of

microtubular proteins arresting cell division• 3)Flucytosine:- Converted to 5-Flurouracil and

compete with Uracil• 4)Azoles :-Alter membrane permeability by

inhibition of ergosterol synthesis• 5)Allylamines:-Inhibits enzyme squalene

epoxide involved in synthesis of ergosterol

• ANTIVIRAL DRUGS• Inhibit Viral attachment and penetration:- Gamma globulins• Inhibitors of viral nucleic acid synthesis• a)Purine analogues:-Acyclovir• b)Pyrimidine analogues:-Zidovudine• c)Pyrophosphate analogues:-Foscarnet• • 3)Inhibitors of viral assembly:- Amantidine• 4)Immunomodulators:-Interferons,Interferon inducers• 5)Miscellaneous • a) Thiosemicarbazones:- Methisazone• b)Antibiotics:-rifampin• c)Others:- Suramin

NSAIDSAnalgesic with antiinflammatory actionClassification:-1. Salicylic acid derivatives :- Aspirin,Sodium salicylate2. Pyrazolone derivative:-

Phenylbutazone,Oxyphenbutazone3. Indole derivative :- Indomethacin,Sulindac4. Oxicam derivative:-Piroxicam,Meloxicam5. Aminonicotinic acid:-Flunixin6. Heteroarylaceticacid derivatives:-

Diclofenac,Ketorolac,Tolmetin.

Analgesic with moderate antiinflammatory action1.Propionicacid derivatives Ibuprofen,Naproxen,Ketoprofen2.Anthranylic acid derivatives :-Meclofenamic acid,Mefenamic

acid3.Sulphonanalidine derivatives:- NimuselideAnalgesics with poor antiinflammatory activity1.Paraaminophenol derivatives:-Paracetamol,Phenacetin2.Pyrazolone derivatives:-Metamizole Selective COX2 inhibitorsEg:- Rofecoxib,CelecoxibACTION:- Inhibit synthesis of prostaglandin.Block cycloxygenase

enzyme

COX 1- Necessary for normal homeostasisCOX2 – Inducible-Inflammation and pain.Side effects are due to

inhibition of COX1Side effects are due to gastric mucosal alteration and bleedingDMSO-Dimehyl sulfoxide-Antiinflammatory

agents,analgesic,antifungal and antimicrobial propertiesOPIOID ANALGESICS

1.Opioid agonists(Natural opium alkaloids)-Morphine,codeine2.Semisynthetic opioids-

Heroin,Hydromorphine,oxymorphine,and etorphine3.Synthetic opioids-

Pethidine,Fentanyl,Diphenoxylate,Loperamide,Methadone,Propoxyphene,Levorphanol,Phenazocin

Mixed agonists- Antagonists and partial antagonists Eg:- Buprenorphine,Pentazocine,Butorphanol,ACTIONInteract with 4 families of opioid receptors such as

µ(mu),δ(Delta),σ(sigma),ǩ(Kappa).CNS –STIMULANTS

1.Psychostimulants/Cerebrostimulants:- Methyl xanthines(Inhibit phosphodiesterase enzyme) Amphetamine,Methylphenidate2.Brain stem stimulants/Analeptics Doxapram,Bemigride,Leptozol,Nikethamide3.Convulscants Strychnine,Brucine,Picrotoxin,Leptozol4.Psychomimetics:- Cannabis,LSD,Mescaline

LOCAL ANAESTHETICS Procaine,Benzocaine,Cocaine,Lignocaine,Prilocaine,Bupivacaine,Mepivacaine

DIURETICS1.High ceiling diuretics/Loop diuretics Frusemide,Ethacrynicacid,Bumetanide2.Mercurials:- Mersalyl3.Thiazide:- Chlorthiazide,Chlorthalidone4.Osmotic diuretic :- Mannitol(Cerebral oedema),Glycerine,Sorbitol and isosorbide4.Carbonic anhydrase inhibitors- Acetezolamide5.Potassium sparing :- Triamterene,Amilioride6.Aldosterone receptor antagonist:- Spironolactone

Acidifying salts:- Ammonium chlorideAlkylating agents:-Potassium acetate,Potassium citrateMethyl Xanthines:- Aminophylline,TheophyllineUrinary alkalinisers:- Sodium bicarbonate,Sodium citrate,Potassium citrate.

SALIVARY STIMULANTSSialagogues/Sialics:- Increases the fluidity and volume of saliva Eg:- Gentian(Dried rhizome and roots of Gentia lutea) Strychnine(Strychnos nuxvomica)Salivary inhibitors/Antisialics:- Reduces salivary secretion Eg:- Atropine,Hyoscine,Glycopyrrolate

DRUGS STIMULATING GASTRIC SECRETIONS1.H2 receptor antagonist:-Cimetidine,Ranitidine,Famotidine2.Proton pump Inhibitors:- (Inactivate H+-K+ ATPase enzyme)

Omperazole,Lansoprazole,Pantoprazole3.Muscarinic receptor antagonists:- Pirezepine,Propantheline4.Prostaglandin Analogues:-MisoprostolACID NEUTRALISING DRUGS1.Systemic antacid:- Sodium bicarbonate,Sodium citrate2.Non systemic antacids:- Al(OH)3,Mg(OH)2

CYTOPROTECTIVE DRUGS1.Sucralfate:- Aluminium salt of sucrose octasulphate.It protects

the ulcerated surface from acid.2.Colloidal Bismuth Subnitrate :- Effective against Helicobacter

pylori.

DRUGS AFFECTING GASTRIC MOTILITY

Prokinetics:- Increases gastric motility1.Dopamine D2 receptor antagonists:- Metaclopromide and Domperidone2. 5HT receptor antagonists:- Cisapride3.H2 receptor antagonists:-Ranitidine, Nizatidine4.Prostaglandins:-Mesoprostol

LAXATIVES AND CATHARTICS1.Lubriacant laxatives:- Liquid paraffin2.Surfactant laxatives:- Docusates3.Simple Bulk prugatives:- Bran,Agar,Methyl cellulose,Carboxymethyl cellulose

4.Osmotic purgatives

a) Inorganic salts:- Mag sulph,Sod sulph b)carbohydrates:- Lactulose,Glycerine,Sorbitol,Mannitol5.Irritant or stimulant purgatives:- a) Direct irritant:- Besacodyl,Phenophthalien b)Indirect irritant purgatives:-Veg oils-Castor oilAnthracene/Anthraquinone purgatives – Aloe,Cascara

sagrada,Senna ,Rhubarb,Danthrone6.Drastic purgatives:- Croton oil7.Neuromuscular purgatives:-

Carbachol,Physostigmine,Arecoloine

ANTIDIARRHOEAL DRUGS1.Gastrointestinal protectants and Adsorbants:-Kaolin,Pectin,Bismuth salts and activated charcoal2.Antimotility Drugs:-Opioids(Tr. Opium,Codiene)3.Antisecretory and antiinflammatory a)Salicylic acid derivatives Sulphasalazine b) Anticholinergic drugs Atropine4.Miscellanoeus drugs:- Tannic acid,Catechu

EMETICS1.Local/Reflex acting emetics:- Sodium chloride,Copper sulphate,Zinc sulphate,Ipecac2.Central acting emetics Apomorphine-Dopamine Antagonist Xylazine α2 agonist

ANTIEMETICSLocal acting:-Demulscents and protectives-

Kaolin,Pectin,Bismuth saltsCentrally acting :- H1 receptor antagnistics:- Meclizine,Cyclizine,Cinnarizine

D2 receptor Antagonistics:-1. Phenothiazine Derivatives:-Chlorpromazine,Acepromazine2. Butorphenones-Droperidol,Haloperidol3. Benzamides:-Metaclopramide5HT3 receptor Antagonist:- Ondansetron,Cyproheptadine.Muscarinic receptor antagonist:- Hyoscine,DicyclomineCARMINATIVESAnise,Asafoetida,Camphor,Cinnamon,Clove,Coriander,Ginger,Pepp

ermint,Menthol

ANTIFOAMING AND ANTI FERMAENTATIVE AGENTS

Turpentine oil mixed with linseed oilFormaline-4ml in 300ml of water tid orally for cattleAntifoaming agents:- Polymerised methylsilicone/Dimethicone,Poloxalene,Arachis oil,Turpentine oil

DRUGS ACTING ON CARDIOVASCULAR SYSTEMMyocardial stimulants 4 groups1. Cardiac glycosides(inhibit Na ,K-ATPase)2.Methyl xanthines3.Bipyridine derivatives eg:-Amrinone and milrinone (also called

‘inodialators’as they areinotropic and vasodialators)4.β agonists like Dobutamine5.Miscellaneous like Calcium and AdrenalineANTIARRHYTHMIC AGENTS-4 groups1.Na channel blockers :- Quinidine,2.Calcium channel blockers:- Verapamil,Diltiazem,Nefidepin3.K channel blockers:-Bretylium and Amiodarone4.β Blocker eg:-Propanalol,satalol,metaprolol

Antihypertensives:-9 groups1.Diuretics:- a) Loop diuretics-Inhibit Na-K-,2 cl- symport b)Thiazide diuretics inhibit Na,K symport c)K sparing diuretics-Spironolactone,Amlioride,Triamterene2.ACE inhibitors:- Captopril,Enalapril3.Angiotensin II receptor antagonists :- Sartans4.Ca channel blockers5.αBlockers:- Prazosin,Phentolamine,Phenoxybutazone6.β blockers :- Propranolol,Atenolol7.Central sympatholytics:- Clonidine (Central α2 agonist)and

Methyl DOPA(False neurotransmitter forms Methyl nor epinephrine)

8.Vasodialators Arteriolar:- Sodium nitroprusside,Organic nitrates(Nitroglycerine)Mixed:-Hydralazine,Minoxidil9.Miscellaneous:- Adrenergic neuron blocker(Reserpine,Guanithidine)Ganglionic blockers(Pentolinium)

HAEMOSTATICSTOPICAL1.Coagulants/clotting factors:- Thrombin,Fibrinogen2.Artificial matrices:_ Fibrin foam,Gelatin sponge3.Vasoconstrictors like adrenaline 4.Styptics/Astringents like FeSO4,Zncl2

SYSTEMIC1.Coagulants a) Vitamin K and Analogues like menadione b) Blood and blood components like whole blood or plasma2.Fibrinolytic inhibitors/Antifibrinolytic agents like Aminocaproic

acid3.Miscellaneous -Protamine sulphate,Adrenochrome,Ethamsylate

ANTIHAEMOSTATICSDrugs used to prevent haemostasis. Divided into 3 groups1.Anticoagulants-In vitro a) Used in labs-Oxalate,NaF,EDTA b)Used for blood coagulation-Na Citrate,ACD,Heparin

IN VIVOa) Parenteral/Rapid acting:- Heparin,Heparinoids- Kefaranb) Oral/Slow acting 1)Coumarin derivatives:-Warfarin 2) Indane dion derivatives:-Phenindione2.Thrombolytics/Fibrinolytics:- Streptokinase ,Urokinase etc3.Antithrombolytics/Antiplatelet drugs:- Aspirin

HAEMATINICS/ANTIANAEMIC DRUGS1.Minerals a) Fe(Iron):- Oral-FeSO4,Ferric ammonium citrate

Parenteral-Fe Dextranb) Copper:- Oral-CuSO4

Parenteral:- Copper Ca edentate,Cu methoxate etcc)Cobalt- CoSO4,CoCl2 etc…

VITAMINS:- B12,B2,B6,Folicacid,Vitamin C etc…Haempoetic growth factorsl ike Erythropoetins/Epoitin(Human

recombinant)HYPOLIPOPROTEINEMIC DRUGS

Are of 5 groups1.HMGCoA Reductase /inhibitors like Statins2.Activators of lipoprotein lipase like

fibrates(Clofibrate,Gemfibrozil)3.Bile acid binding resins like Colistipol4.CETP Imhibitors(Cholesteryl ester transfer protein) Like

Torcetrapib4.Miscellaneous likeB3 or gugulipidor Omega 3 fatty acids

CNS PHARMACOLOGYEther was first used byWilliam.T.G.Morgan-1846Choloroform was introduced by James Simpson in 1847GENERAL ANAESTHETICSMainly 2 groupsInhalent 1.Non gaseous/Volatile:- Halothane,Ether,Chloroform2.Gaseous:-N2O,Xenon,CyclopropaneInjectable 1.Barbiturate2.Dissociative3.Non Barbiturate – Non dissociative Eg:- Propofol,Saffan,Chloral hydrate

SEDATIVES/HYPNOTIC SEDATIVES-7Groups1.Benzodiazepines2.α2 Agonists:- Xylazines,Detomidine etc….3.Barbiturates4.Chloral Derivatives:- Chloral hydrate (In olden days)5.Aldehydes:- Paraldehydes6.Inorganic salts:- NBr,KBr,etc7.Miscellaneous – Ethyl alcohol BARBITURATES 4 groups1.Ultrashort acting-Thiopentone2.Short acting-Pento and seco barbitone3.Intermediate acting –Amo,Apr,Mephobarbitone4.Long acting –Barbitone,Pheno and Butabarbitone

TRANQUILISERS:- Mainly 3 groups1.Phenothiazene like Chlorpromazines and Acepromazines2.Thioxanthines:- Chlorprothixene3.Butyrophenones:- Azaperone,Droperidol etcMOA of Benzodiazepines:- GABA facilitator actionMOA of Barbiturates:-GABA actionANTICONVULSCENTS 1.Barbiturates-Pheno,Pentoand mephobarbitone2.Deoxybarbiturate-Prinidone3.Hydantoins-Phenytion,Mephenytion4.Benzodiazepines-Clonazepam,Diazepam5.Aliphatic carboxylic acids:- Valproic acids6.Bromides (7) Succimides eg:- Ethosuccimide,Methosuccimide8.Newer agents:- Gabaprotein,Toperamate