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Essentials of Medical Pharmacology
KD Tripathi
SECTION 1: GENERAL PHARMACOLOGICAL PRINCIPLES
CHAPTER 1:
Introduction, Routes of Drug Administration
INTRODUCTION
Pharmacology
DRUG NOMENCLATURE
ESSENTIAL DRUGS (MEDICINES) CONCEPT
ROUTES OF DRUG ADMINISTRATION
LOCAL ROUTES
SYSTEMIC ROUTES
1. Oral
2. Sublingual (s.l.) or buccal
3. Rectal
4. Cutaneous
5. Inhalation
6. Nasal
7. Parenteral
CHAPTER 2:
Pharmacokinetics: Membrane Transport, Absorption and Distribution of Drugs
ABSORPTION
Oral
Subcutaneous and Intramuscular
Topical sites (skin, cornea, mucous membranes)
BIOAVAILABILITY
DISTRIBUTION
Plasma protein binding
CHAPTER 3:
Pharmacokinetics: Metabolism and Excretion of Drugs, Kinetics of Elimination
BIOTRANSFORMATION (Metabolism)
Nonsynthetic reactions
Synthetic reactions
INHIBITION OF DRUG METABOLISM
MICROSOMAL ENZYME INDUCTION
Consequences of microsomal enzyme induction
Possible uses of enzyme induction
FIRST PASS (PRESYSTEMIC) METABOLISM
EXCRETION
RENAL EXCRETION
KINETICS OF ELIMINATION
Repeated drug administration
Plateau principle
Monitoring of plasma concentration is of no value for
PROLONGATION OF DRUG ACTION
CHAPTER 4:
Pharmacodynamics: Mechanism of Drug Action; Receptor Pharmacology
PRINCIPLES OF DRUG ACTION
MECHANISM OF DRUG ACTION
I. ENZYMES
II. ION CHANNELS
III. TRANSPORTERS
IV. RECEPTORS
Basic evidences for drug action through receptors
Receptor occupation theory
The two-state receptor model
Nature of receptors
Receptor subtypes
ACTION-EFFECT SEQUENCE
TRANSDUCER MECHANISMS
1. G-protein coupled receptors (GPCR)
2. Receptors with intrinsic ion channel
3. Enzyme-linked receptors
4. Receptors regulating gene expression (Transcription factors)
Receptor regulation
Nonreceptor-mediated drug action
DOSE-RESPONSE RELATIONSHIP
Therapeutic window phenomenon
Drug potency and efficacy
Selectivity
COMBINED EFFECT OF DRUGS
SYNERGISM
ANTAGONISM
CHAPTER 5:
Aspects of Pharmacotherapy; Clinical Pharmacology and Drug Development
DRUG DOSAGE
Fixed dose ratio combination preparations
FACTORS MODIFYING DRUG ACTION
RATIONAL USE OF MEDICINES
Rational prescribing
Information/instructions to the patient
EXPIRY DATE OF PHARMACEUTICALS
EVIDENCE BASED MEDICINE
Clinical trial
Sequential trial
Meta-analysis
Cohort study
Case control study
NEW DRUG DEVELOPMENT
Approaches to drug discovery
Preclinical studies
Clinical trials
Phase I: Human pharmacology and safety
Phase II: Therapeutic exploration and dose ranging
Phase III: Therapeutic confirmation/comparison
Phase IV: Postmarketing surveillance/studies
CHAPTER 6:
Adverse Drug Effects
SECTION 2: DRUGS ACTING ON AUTONOMIC NERVOUS SYSTEM
CHAPTER 7:
Cholinergic System and Drugs
CHOLINERGIC TRANSMISSION
Synthesis, storage and destruction of ACh
Cholinoceptors
CHOLINERGIC DRUGS (Cholinomimetic, Parasympathomimetic)
CHOLINERGIC AGONISTS
ACTIONS (of ACh as prototype)
A. Muscarinic
B. Nicotinic
C. CNS
CHOLINOMIMETIC ALKALOIDS
ANTICHOLINESTERASES
Reversible
Irreversible
CHEMISTRY
MECHANISM OF ACTION
PHARMACOLOGICAL ACTIONS
PHARMACOKINETICS
INDIVIDUAL COMPOUNDS
USES
1. As miotic
2. Myasthenia gravis
Diagnostic tests for myasthenia gravis
ANTICHOLINESTERASE POISONING
Treatment
CHAPTER 8:
Anticholinergic Drugs and Drugs Acting on Autonomic Ganglia
ANTICHOLINERGIC DRUGS (Muscarinic receptor antagonists, Atropinic, Parasympatholytic)
CLASSIFICATION
PHARMACOLOGICAL ACTIONS (Atropine as prototype)
PHARMACOKINETICS
ATROPINE SUBSTITUTES
Quaternary compounds
Tertiary amines
Vasicoselective drugs
Mydriatics
Antiparkinsonian drugs (see Ch. 31)
USES
I. As antisecretory
II. As antispasmodic
III. Bronchial asthma, asthmatic bronchitis, COPD
IV. As mydriatic and cycloplegic
V. As cardiac vagolytic
VI. For central action
VII. To antagonise muscarinic effects of drugs and poisons
SIDE EFFECTS AND TOXICITY
Interactions
DRUGS ACTING ON AUTONOMIC GANGLIA
Ganglionic stimulants
Ganglion blocking agents
CHAPTER 9:
Adrenergic System and Drugs
ADRENERGIC TRANSMISSION
ADRENERGIC DRUGS (Sympathomimetics)
ACTIONS
Biochemical mediation of adrenergic responses
Administration and preparations
Adverse effects and contraindications
THERAPEUTIC CLASSIFICATION OF ADRENERGIC DRUGS
SELECTIVE β2 STIMULANTS
NASAL DECONGESTANTS
ANORECTIC AGENTS
THERAPEUTIC USES
1. Vascular Uses
2. Cardiac uses
6. Central uses
CHAPTER 10:
Antiadrenergic Drugs (Adrenergic Receptor Antagonists) and Drugs for Glaucoma
α ADRENERGIC BLOCKING drugs
CLASSIFICATION
GENERAL EFFECTS OF α BLOCKERS
USES OF α BLOCKERS
β ADRENERGIC BLOCKING DRUGS
CLASSIFICATION
PHARMACOLOGICAL ACTIONS
1. CVS
PHARMACOKINETICS
INTERACTIONS
ADVERSE EFFECTS AND CONTRAINDICATIONS
OTHER β BLOCKERS
USES
α + β ADRENERGIC BLOCKERS
DRUGS FOR GLAUCOMA
A. Open angle (wide angle, chronic simple) glaucoma
1. β Adrenergic blockers
2. α Adrenergic agonists
3. Prostaglandin analogues
4. Carbonic anhydrase inhibitors
B. Angle closure (narrow angle, acute congestive) glaucoma
SECTION 3: AUTACOIDS AND RELATED DRUGS
CHAPTER 11:
Histamine and Antihistaminics
HISTAMINE
PHARMACOLOGICAL ACTIONS
PATHOPHYSIOLOGICAL ROLES
USES
HISTAMINE RELEASERS
H1 ANTAGONISTS (Conventional antihistaminics)
PHARMACOLOGICAL ACTIONS
PHARMACOKINETICS
SIDE EFFECTS AND TOXICITY
SECOND GENERATION ANTIHISTAMINICS
USES
DRUGS FOR VERTIGO
CHAPTER 12:
5-Hydroxytryptamine, its Antagonists and Drug Therapy of Migraine
5-HYDROXYTRYPTAMINE (5-HT, Serotonin)
SYNTHESIS, STORAGE AND DESTRUCTION
Serotonergic (5-HT) Receptors
ACTIONS
PATHOPHYSIOLOGICAL ROLES
DRUGS AFFECTING 5-HT SYSTEM
5-HT ANTAGONISTS
ERGOT ALKALOIDS
Other semisynthetic derivatives
Actions
DRUG THERAPY OF MIGRAINE
SELECTIVE 5-HT1B/1D AGONISTS
Prophylaxis of migraine
CHAPTER 13:
Prostaglandins, Leukotrienes (Eicosanoids) and Platelet Activating Factor
PROSTAGLANDINS AND LEUKOTRIENES (Eicosanoids)
CHEMISTRY, BIOSYNTHESIS AND DEGRADATION
ACTIONS AND PATHOPHYSIOLOGICAL ROLES
Prostaglandins, thromboxanes and prostacyclin
Leukotrienes
PROSTANOID RECEPTORS
LEUKOTRIENE RECEPTORS
USES
SIDE EFFECTS
PLATELET ACTIVATING FACTOR (PAF)
CHAPTER 14:
Nonsteroidal Antiinflammatory Drugs and Antipyretic-Analgesics
CLASSIFICATION
A. Nonselective COX inhibitors (traditional NSAIDs)
B. Preferential COX-2 inhibitors
C. Selective COX-2 inhibitors
D. Analgesic-antipyretics with poor antiinflammatory action
NSAIDs and prostaglandin (PG) synthesis inhibition
SALICYLATES
PHARMACOLOGICAL ACTIONS
PHARMACOKINETICS
ADVERSE EFFECTS
Precautions and contraindications
Interactions
USES
PROPIONIC ACID DERIVATIVES
ANTHRANILIC ACID DERIVATIVE (FENAMATE)
ARYL-ACETIC ACID DERIVATIVES
OXICAM DERIVATIVES
PYRROLO-PYRROLE DERIVATIVE
INDOLE DERIVATIVE
PYRAZOLONES
PREFERENTIAL COX-2 INHIBITORS
SELECTIVE COX-2 INHIBITORS (Coxibs)
PARA-AMINO PHENOL DERIVATIVES
BENZOXAZOCINE DERIVATIVE
Preparations
Choice of nonsteroidal antiinflammatory drug
Analgesic combinations
CHAPTER 15:
Antirheumatoid and Antigout Drugs
ANTIRHEUMATOID DRUGS
A. Disease modifying antirheumatic drugs (DMARDs)
B. Biologic response modifiers (BRMs)
C. Adjuvant drugs
1. Immunosuppressants (see Ch. 63)
2. Sulfasalazine (see Ch. 48)
3. Chloroquine and hydroxychloroquine (see Ch. 59)
4. Leflunomide
5. Gold
6. d-Penicillamine
7. Biologic response modifiers
TNFα inhibitors
IL-1 antagonist
8. Corticosteroids (see Ch. 20)
DRUGS USED IN GOUT
ACUTE GOUT
1. NSAIDs
2. Colchicine
3. Corticosteroids
CHRONIC GOUT
A. URICOSURIC DRUGS
1. Probenecid
2. Sulfinpyrazone
B. URIC ACID SYNTHESIS INHIBITOR
Allopurinol
SECTION 4: RESPIRATORY SYSTEM DRUGS
CHAPTER 16:
Drugs for Cough and Bronchial Asthma
DRUGS FOR COUGH
DEMULCENTS AND EXPECTORANTS
Mucolytics
ANTITUSSIVES
Opioids
Nonopioids
Antihistamines
SOME ANTITUSSIVE-EXPECTORANT COMBINATIONS
DRUGS FOR BRONCHIAL ASTHMA
APPROACHES TO TREATMENT
CLASSIFICATION
SYMPATHOMIMETICS (see Ch. 9)
METHYL XANTHINES
Pharmacological actions
Theophylline
Preparations and dose
ANTICHOLINERGICS (see Ch. 8)
LEUKOTRIENE ANTAGONISTS
MAST CELL STABILIZERS
Sodium cromoglycate (Cromolyn sod.)
CORTICOSTEROIDS
SYSTEMIC STEROID THERAPY
INHALED STEROIDS
ANTI-IgE ANTIBODY
INHALED ASTHMA MEDICATION
CHOICE OF TREATMENT
Some antiasthma combinations
SECTION 5: HORMONES AND RELATED DRUGS
CHAPTER 17:
Anterior Pituitary Hormones
GROWTH HORMONE (GH)
GH Inhibitors
Somatostatin
PROLACTIN
Prolactin inhibitors
Bromocriptine
Actions
Cabergoline
GONADOTROPINS (Gns)
Preparations
Uses
Adverse effects and precautions
THYROID STIMULATING HORMONE (TSH, THYROTROPIN)
ADRENOCORTICOTROPIC HORMONE (ACTH, CORTICOTROPIN)
CHAPTER 18:
Thyroid Hormones and Thyroid Inhibitors
THYROID HORMONE
CHEMISTRY AND SYNTHESIS
TRANSPORT, METABOLISM AND EXCRETION
REGULATION OF SECRETION
ACTIONS
Mechanism of action
Relation between T4 and T3
Preparations
USES
THYROID INHIBITORS
CLASSIFICATION
ANTITHYROID DRUGS
Preparations and dose
IONIC INHIBITORS
IODINE AND IODIDES
Uses
Adverse effects
RADIOACTIVE IODINE
β ADRENERGIC BLOCKERS
CHAPTER 19:
Insulin, Oral Hypoglycaemic Drugs and Glucagon
INSULIN
Regulation of insulin secretion
ACTIONS OF INSULIN
Conventional preparations of insulin
Highly purified insulin preparations
Insulin analogues
REACTIONS TO INSULIN
Drug interactions
USES OF INSULIN
Insulin resistance
ORAL HYPOGLYCAEMIC DRUGS
SULFONYLUREAS
BIGUANIDES
MEGLITINIDE / PHENYL ALANINE ANALOGUES
THIAZOLIDINEDIONES
α GLUCOSIDASE INHIBITORS
SULFONYLUREAS
Interactions
BIGUANIDES
MEGLITINIDE / D-PHENYLALANINE ANALOGUES
THIAZOLIDINEDIONES
α GLUCOSIDASE INHIBITORS
Status of oral hypoglycaemics in diabetes mellitus
NEWER APPROACHES IN DIABETES
GLUCAGON
Uses
Other hyperglycaemics
CHAPTER 20:
Corticosteroids
BIOSYNTHESIS
ACTIONS
Mineralocorticoid actions
Glucocorticoid actions
Mechanism of action at cellular level
PHARMACOKINETICS
CHEMISTRY AND RELATIVE ACTIVITY OF CORTICOIDS
DISTINCTIVE FEATURES
USES
ADVERSE EFFECTS
CONTRAINDICATIONS
CHAPTER 21:
Androgens and Drugs for Erectile Dysfunction
ANDROGENS(Male Sex Hormones)
Regulation of secretion
ACTIONS
Mechanism of action
PHARMACOKINETICS
Preparations and Dose
SIDE EFFECTS
USES
ANABOLIC STEROIDS
Preparations and dose
Uses
IMPEDED ANDROGENS / ANTIANDROGENS
5 α-REDUCTASE INHIBITOR
DRUGS FOR ERECTILE DYSFUNCTION
1. Androgens
2. Phosphodiesterase-5 (PDE-5) inhibitors
3. Papaverine/Phentolamine induced penile erection (PIPE) therapy
4. Prostaglandin E1
CHAPTER 22:
Estrogens, Progestins and Contraceptives
ESTROGENS(Female Sex Hormones)
ACTIONS
Mechanism of action
PHARMACOKINETICS
Preparations and dose
ADVERSE EFFECTS
USES
Hormone replacement therapy (HRT)
ANTIESTROGENS AND SELECTIVE ESTROGEN RECEPTOR MODULATORS (SERMs)
Antiestrogens
Selective estrogen receptor modulators (SERMs)
AROMATASE INHIBITORS
PROGESTINS
ACTIONS
Mechanism of action
PHARMACOKINETICS
Preparations and dose
ADVERSE EFFECTS
USES
ANTIPROGESTIN
Uses
HORMONAL CONTRACEPTIVES
FEMALE CONTRACEPTION
TYPES OF METHODS
Oral
Injectable
MECHANISM OF ACTION
Practical considerations
ADVERSE EFFECTS
Contraindications
MALE CONTRACEPTIVE
CHAPTER 23:
Oxytocin and Other Drugs Acting on Uterus
UTERINE STIMULANTS (Oxytocics, Abortifacients)
OXYTOCIN
ACTIONS
Physiological role
PHARMACOKINETICS
USE
Adverse effects
ERGOMETRINE, METHYLERGOMETRINE
Use
PROSTAGLANDINS
UTERINE RELAXANTS (Tocolytics)
CHAPTER 24:
Drugs Affecting Calcium Balance
CALCIUM
Physiological roles
Preparations
Use
PARATHYROID HORMONE (Parathormone)
Actions
CALCITONIN
Actions
Uses
VITAMIN D
Actions
Pharmacokinetics
Unitage and preparations
Use
Interactions
BISPHOSPHONATES
Other drugs for hypercalcaemia
SECTION 6: DRUGS ACTING ON PERIPHERAL (SOMATIC) NERVOUS SYSTEM
CHAPTER 25:
Skeletal Muscle Relaxants
PERIPHERALLY ACTING MUSCLE RELAXANTS
I. Neuromuscular blocking agents
A. Nondepolarizing (Competitive) blockers
B. Depolarizing blockers
II. Directly acting agents
NEUROMUSCULAR BLOCKING AGENTS
MECHANISM OF ACTION
ACTIONS
PHARMACOKINETICS
NOTES ON INDIVIDUAL COMPOUNDS
INTERACTIONS
TOXICITY
USES
DIRECTLY ACTING MUSCLE RELAXANTS
CENTRALLY ACTING MUSCLE RELAXANTS
CLASSIFICATION
Uses of centrally acting muscle relaxants
CHAPTER 26:
Local Anaesthetics
CLASSIFICATION
Injectable anaesthetic
Surface anaesthetic
CHEMISTRY
MECHANISM OF ACTION
LOCAL ACTIONS
SYSTEMIC ACTIONS
C.N.S.
C.V.S.
PHARMACOKINETICS
ADVERSE EFFECTS
Precautions and interactions
INDIVIDUAL COMPOUNDS
USES AND TECHNIQUES OF LOCAL ANAESTHESIA
Complications of spinal anaesthesia
SECTION 7: DRUGS ACTING ON CENTRAL NERVOUS SYSTEM
CHAPTER 27:
General Anaesthetics
MECHANISM OF GENERAL ANAESTHESIA
STAGES OF ANAESTHESIA
PHARMACOKINETICS OF INHALATIONAL ANAESTHETICS
TECHNIQUES OF INHALATION OF ANAESTHETICS
Properties of an ideal anaesthetic
CLASSIFICATION
Inhalational
Intravenous
INHALATIONAL ANAESTHETICS
INTRAVENOUS ANAESTHETICS
INDUCING AGENTS
SLOWER ACTING DRUGS
CONSCIOUS SEDATION
COMPLICATIONS OF GENERAL ANAESTHESIA
A. During anaesthesia
B. After anaesthesia
DRUG INTERACTIONS
PREANAESTHETIC MEDICATION
CHAPTER 28:
Ethyl and Methyl Alcohols
ETHYL ALCOHOL (Ethanol)
ALCOHOLIC BEVERAGES
Other forms of alcohol
PHARMACOLOGICAL ACTIONS
PHARMACOKINETICS
INTERACTIONS
Food value
CONTRAINDICATIONS
TOXICITY
CLINICAL USES
Aldehyde dehydrogenase inhibitors
METHYL ALCOHOL (Methanol, Wood alcohol)
Treatment
CHAPTER 29:
Sedative-Hypnotics
CLASSIFICATION
2. Benzodiazepines
3. Newer nonbenzodiazepine hypnotics
BARBITURATES
PHARMACOLOGICAL ACTIONS
2. Other systems
PHARMACOKINETICS
USES
ADVERSE EFFECTS
Contraindications
Interactions
BENZODIAZEPINES (BZDs)
Site and mechanism of action
PHARMACOKINETICS
I. Slow elimination of parent drug or active metabolite
II. Relatively slow elimination but marked redistribution
III. Relatively rapid elimination and marked redistribution
IV. Ultrarapid elimination
ADVERSE EFFECTS
INTERACTIONS
NON-BENZODIAZEPINE HYPNOTICS
USES
2. Other uses
BENZODIAZEPINE ANTAGONIST
Uses
CHAPTER 30:
Antiepileptic Drugs
CLASSIFICATION
Phenobarbitone (see Ch. 29)
Phenytoin (Diphenylhydantoin)
At therapeutic levels
At high plasma levels (dose related toxicity)
Carbamazepine
Ethosuximide
Valproic acid (Sodium valproate)
Interactions
Clonazepam
Diazepam (see Ch. 29)
TREATMENT OF EPILEPSIES
CHAPTER 31:
Antiparkinsonian Drugs
CLASSIFICATION
LEVODOPA
ACTIONS
PHARMACOKINETICS
ADVERSE EFFECTS
After prolonged therapy
Interactions
PERIPHERAL DECARBOXYLASE INHIBITORS
Preparations and dose
DOPAMINERGIC AGONISTS
MAO-B INHIBITOR
COMT INHIBITORS
DOPAMINE FACILITATOR
CENTRAL ANTICHOLINERGICS
Some general points
CHAPTER 32:
Drugs Used in Mental Illness: Antipsychotic and Antimanic Drugs
ANTIPSYCHOTIC DRUGS(Neuroleptics)
CLASSIFICATION
PHARMACOLOGICAL ACTIONS
Tolerance and dependence
PHARMACOKINETICS
DISTINCTIVE FEATURES OF NEUROLEPTICS
ATYPICAL ANTIPSYCHOTICS
ADVERSE EFFECTS
I. Based on pharmacological actions (dose related)
INTERACTIONS
USES
ANTIMANIC (MOOD STABILIZING) DRUGS
LITHIUM CARBONATE
Actions and mechanism
Pharmacokinetics and control of therapy
Interactions
use
ALTERNATIVES TO LITHIUM
HALLUCINOGENS (Psychotomimetics, Psychedelics, Psychodysleptics, Psychotogens)
INDOLE AMINES
PHENYLALKYLAMINES
ARYLCYCLOHEXYL AMINES
CANNABINOIDS
CHAPTER 33:
Drugs Used in Mental Illness: Antidepressant and Antianxiety Drugs
ANTIDEPRESSANTS
CLASSIFICATION
MAO INHIBITORS
Nonselective MAO Inhibitors
Reversible inhibitors of MAO-A (RIMAs)
TRICYCLIC ANTIDEPRESSANTS (TCAs)
PHARMACOLOGICAL ACTIONS
Tolerance and dependence
PHARMACOKINETICS
INTERACTIONS
SELECTIVE SEROTONIN REUPTAKE INHIBITORS (SSRIs)
ATYPICAL ANTIDEPRESSANTS
USES
ANTIANXIETY DRUGS
CLASSIFICATION
BENZODIAZEPINES
OTHER ANTIANXIETY DRUGS
β Blockers (see Ch. 10)
TREATMENT OF ANXIETY
CHAPTER 34:
Opioid Analgesics and Antagonists
OPIOID ANALGESICS
MORPHINE
PHARMACOLOGICAL ACTIONS
PHARMACOKINETICS
ADVERSE EFFECTS
PRECAUTIONS AND CONTRAINDICATIONS
Interactions
CLASSIFICATION OF OPIOIDS
USES (Of Morphine and its congeners).
OPIOID RECEPTORS
COMPLEX ACTION OPIOIDS AND OPIOID ANTAGONISTS
PURE OPIOID ANTAGONISTS
ENDOGENOUS OPIOID PEPTIDES
CHAPTER 35:
CNS Stimulants and Cognition Enhancers
CNS STIMULANTS
CLASSIFICATION
I. CONVULSANTS
II. ANALEPTICS (Respiratory stimulants)
III. PSYCHOSTIMULANTS
5. Cocaine (see Ch. 26)
Uses
COGNITION ENHANCERS (Cerebroactive drugs)
SECTION 8: CARDIOVASCULAR DRUGS
CHAPTER 36:
Drugs Affecting Renin-Angiotensin System and Plasma Kinins
ANGIOTENSIN
ACTIONS
PATHOPHYSIOLOGICAL ROLES
ANGIOTENSIN CONVERTING ENZYME INHIBITORS
Captopril
OTHER ACE INHIBITORS
USES
ANGIOTENSIN ANTAGONISTS(Angiotensin receptor blockers or ARBs)
Uses of AT1 receptor antagonists (ARBs)
PLASMA KININS (Bradykinin and Kallidin)
ACTIONS
PATHOPHYSIOLOGICAL ROLES
Bradykinin antagonists
CHAPTER 37:
Cardiac Glycosides and Drugs for Heart Failure
CARDIAC GLYCOSIDES
CHEMISTRY
PHARMACOLOGICAL ACTIONS
PHARMACOKINETICS
Preparations
ADVERSE EFFECTS
PRECAUTIONS AND CONTRAINDICATIONS
INTERACTIONS
USES
1. Congestive heart failure
2. Cardiac arrhythmias
TREATMENT OF CHF
Diuretics
Vasodilators
Sympathomimetic inotropic drugs (see Ch. 9)
Phosphodiesterase III inhibitors
CHAPTER 38:
Antiarrhythmic Drugs
CLASSIFICATION
CLASS I
SUBCLASS IA
Quinidine
Procainamide
Disopyramide
SUBCLASS IB
Lidocaine (Lignocaine)
Mexiletine
SUBCLASS IC
CLASS II
CLASS III
Amiodarone
CLASS IV
Verapamil
Uses and precautions
Drugs for PSVT
Adenosine
Other uses of adenosine
Drugs for A-V Block
Choice of antiarrhythmics
CHAPTER 39:
Antianginal and Other Anti-ischaemic Drugs
ANTIANGINAL DRUGS
CLASSIFICATION
NITRATES (GTN as prototype)
INDIVIDUAL DRUGS
USES
β BLOCKERS (see Ch. 10)
CALCIUM CHANNEL BLOCKERS
Calcium channels
PHARMACOLOGICAL ACTIONS AND ADVERSE EFFECTS
Other dihydropyridines (DHPs)
PHARMACOKINETICS
USES
RATIONAL DRUG COMBINATIONS
POTASSIUM CHANNEL OPENERS
OTHER ANTIANGINAL DRUGS
DRUGS FOR PERIPHERAL VASCULAR DISEASES
DRUG THERAPY IN MYOCARDIAL INFARCTION
CHAPTER 40:
Antihypertensive Drugs
CLASSIFICATION
DIURETICS
ANGIOTENSIN CONVERTING ENZYME (ACE) INHIBITORS
ANGIOTENSIN RECEPTOR BLOCKERS
CALCIUM CHANNEL BLOCKERS
β-ADRENERGIC BLOCKERS
β+α ADRENERGIC BLOCKERS
α-ADRENERGIC BLOCKERS
Prazosin (see Ch. 10)
Nonselective α blockers (Phentolamine, Phenoxybenzamine)
CENTRAL SYMPATHOLYTICS
VASODILATORS
ADRENERGIC NEURONE BLOCKERS
TREATMENT OF HYPERTENSION
Combinations to be avoided
Some antihypertensive combinations
Antihypertensives to be avoided during pregnancy
Antihypertensives found safer during pregnancy
Hypertensive emergencies and urgencies
SECTION 9: DRUGS ACTING ON KIDNEY
CHAPTER 41:
Diuretics
CLASSIFICATION
HIGH CEILING (LOOP) DIURETICS
Use of high ceiling diuretics
THIAZIDE AND RELATED DIURETICS
Uses
Complications of high ceiling and thiazide type diuretic therapy
Interactions
CARBONIC ANHYDRASE INHIBITORS
Acetazolamide
POTASSIUM SPARING DIURETICS
Spironolactone (Aldosterone antagonist)
Interactions
Inhibitors of renal epithelial Na+ channel
OSMOTIC DIURETICS
Mannitol
CHAPTER 42:
Antidiuretics
ANTIDIURETIC HORMONE
ADH (Vasopressin) receptors
Actions
VASOPRESSIN ANALOGUES
Uses
THIAZIDES
SECTION 10: DRUGS AFFECTING BLOOD AND BLOOD FORMATION
CHAPTER 43:
Haematinics and Erythropoietin
IRON
Iron absorption
Factors facilitating iron absorption
Factors impeding iron absorption
Transport, utilization, storage and excretion
Preparations and dose
Oral iron
Parenteral iron
Adverse effects of parenteral iron
use
ACUTE IRON POISONING
To prevent further absorption of iron from gut
To bind and remove iron already absorbed
Miscellaneous/Adjuvant haematinics
MATURATION FACTORS
VITAMIN-B12
Preparations, dose, administration
Uses
FOLIC ACID
Preparations and dose
Uses
ERYTHROPOIETIN
CHAPTER 44:
Drugs Affecting Coagulation, Bleeding and Thrombosis
COAGULANTS
VITAMIN K
Preparations
LOCAL HAEMOSTATICS (STYPTICS)
SCLEROSING AGENTS
ANTICOAGULANTS
I. Used in vivo
II. Used in vitro
HEPARIN
ACTIONS
PHARMACOKINETICS
ADVERSE EFFECTS
Contraindications
Low molecular weight (LMW) heparins
HEPARINOIDS
HEPARIN ANTAGONIST
ORAL ANTICOAGULANTS
Action and mechanism
USES OF ANTICOAGULANTS
FIBRINOLYTICS(Thrombolytics)
Uses of fibrinolytics
ANTIFIBRINOLYTICS
ANTIPLATELET DRUGS(Antithrombotic drugs)
Glycoprotein (GP) IIb/IIIa receptor antagonists
Uses of antiplatelet drugs
CHAPTER 45:
Hypolipidaemic Drugs and Plasma Expanders
HYPOLIPIDAEMIC DRUGS
Lipid transport
CLASSIFICATION
HMG-CoA REDUCTASE INHIBITORS (STATINS)
BILE ACID SEQUESTRANTS (RESINS)
FIBRIC ACID DERIVATIVES
NICOTINIC ACID (NIACIN)
OTHER HYPOLIPIDAEMICS
Comments on the use of hypolipidaemic drugs
PLASMA EXPANDERS
USE OF PLASMA EXPANDERS
SECTION 11: GASTROINTESTINAL DRUGS
CHAPTER 46:
Drugs for Peptic Ulcer
H2 ANTAGONISTS
PHARMACOLOGICAL ACTIONS
PHARMACOKINETICS
ADVERSE EFFECTS
INTERACTIONS
USES
PROTON PUMP INHIBITORS (PPIs)
Uses
ANTICHOLINERGICS (See Ch. 8)
PROSTAGLANDIN ANALOGUE
ANTACIDS
SYSTEMIC ANTACIDS
NONSYSTEMIC ANTACIDS
Uses
ULCER PROTECTIVES
Colloidal bismuth subcitrate (CBS; Tripotassium dicitratobismuthate)
ANTI-HELICOBACTER PYLORI DRUGS
Role of drugs in peptic ulcer disease
CHAPTER 47:
Drugs for Emesis, Reflux and Digestive Disorders
EMETICS
ANTIEMETICS
CLASSIFICATION
ANTICHOLINERGICS (See Ch. 8)
H1 ANTIHISTAMINICS (See Ch. 11)
NEUROLEPTICS (see Ch. 32)
PROKINETIC DRUGS
Metoclopramide
Actions
Uses
5-HT3 ANTAGONISTS
ADJUVANT ANTIEMETICS
Gastroesophageal reflux disease (GERD)
CARMINATIVES
DIGESTANTS
Preparations
GALLSTONE DISSOLVING DRUGS
CHAPTER 48:
Drugs for Constipation and Diarrhoea
LAXATIVES (Aperients, Purgatives, Cathartics)
CLASSIFICATION
MECHANISM OF ACTION
BULK PURGATIVES
STOOL SOFTENER
STIMULANT PURGATIVES
Diphenylmethanes
Anthraquinones
Castor oil
OSMOTIC PURGATIVES
CHOICE AND USE OF PURGATIVES
Some combined preparations
TREATMENT OF DIARRHOEAS
Relevant pathophysiology
Principles of management
REHYDRATION
Rationale of ORS composition
Non-diarrhoeal uses of ORT
MAINTENANCE OF NUTRITION
DRUG THERAPY
ANTIMICROBIALS
B. Antimicrobials are useful only in severe disease (but not in mild cases):
C. Antimicrobials are regularly useful in:
NONSPECIFIC ANTIDIARRHOEAL AGENTS
2. Antisecretory drugs
Immunosuppressants (see Ch. 63)
3. Antimotility drugs
SECTION 12: ANTIMICROBIAL DRUGS
CHAPTER 49:
Antimicrobial Drugs: General Considerations
CLASSIFICATION
A. Chemical structure
B. Mechanism of action
C. Type of organisms against which primarily active
D. Spectrum of activity
E. Type of action
F. Antibiotics are obtained from:
PROBLEMS THAT ARISE WITH THE USE OF AMAs
1. Toxicity
2. Hypersensitivity reactions
3. Drug resistance
4. Superinfection (Suprainfection)
5. Nutritional deficiencies
6. Masking of an infection
CHOICE OF AN ANTIMICROBIAL AGENT
Patient factors
Organism-related considerations
Drug factors
COMBINED USE OF ANTIMICROBIALS
Disadvantages of antimicrobial combinations
PROPHYLACTIC USE OF ANTIMICROBIALS
Prophylaxis of surgical site infection
FAILURE OF ANTIMICROBIAL THERAPY
CHAPTER 50:
Sulfonamides, Cotrimoxazole and Quinolones
SULFONAMIDES
ANTIBACTERIAL SPECTRUM
PHARMACOKINETICS
ADVERSE EFFECTS
USES
COTRIMOXAZOLE
Uses
QUINOLONES
Nalidixic acid
Use
FLUOROQUINOLONES
Ciprofloxacin (prototype)
Interactions
CHAPTER 51:
Beta-Lactam Antibiotics
PENICILLINS
Mechanism of action
PENICILLIN-G (BENZYL PENICILLIN)
Pharmacokinetics
Preparations and dose
Adverse effects
Uses
SEMISYNTHETIC PENICILLINS
CLASSIFICATION
ACID-RESISTANT ALTERNATIVE TO PENICILLIN-G
Phenoxymethyl penicillin (Penicillin V)
PENICILLINASE-RESISTANT PENICILLINS
EXTENDED SPECTRUM PENICILLINS
1. Aminopenicillins
Uses
2. Carboxypenicillins
3. Ureidopenicillins
BETA-LACTAMASE INHIBITORS
CEPHALOSPORINS
FIRST GENERATION CEPHALOSPORINS
SECOND GENERATION CEPHALOSPORINS
THIRD GENERATION CEPHALOSPORINS
FOURTH GENERATION CEPHALOSPORINS
Adverse effects
Uses
MONOBACTAMS
CARBAPENEMS
CHAPTER 52:
Tetracyclines and Chloramphenicol (Broad-Spectrum Antibiotics)
TETRACYCLINES
Pharmacokinetics
Preparations
Adverse effects
Dose related toxicity
Precautions
Uses
CHLORAMPHENICOL
Pharmacokinetics
Preparations and administration
Adverse effects
Uses
CHAPTER 53:
Aminoglycoside Antibiotics
MECHANISM OF ACTION
MECHANISM OF RESISTANCE
SHARED TOXICITIES
PRECAUTIONS AND INTERACTIONS
STREPTOMYCIN
Uses
GENTAMICIN
KANAMYCIN
TOBRAMYCIN
AMIKACIN
SISOMICIN
NETILMICIN
NEOMYCIN
FRAMYCETIN
CHAPTER 54:
Macrolide, Lincosamide, Glycopeptide and Other Antibacterial Antibiotics; Urinary Antiseptics
MACROLIDE ANTIBIOTICS
ERYTHROMYCIN
Pharmacokinetics
Preparations and dose
Uses
A. As an alternative to penicillin
B. As a first choice drug for
C. As a second choice drug in
NEWER MACROLIDES
LINCOSAMIDE ANTIBIOTICS
Clindamycin
Lincomycin
GLYCOPEPTIDE ANTIBIOTICS
Vancomycin
OXAZOLIDINONE
Fusidic acid
POLYPEPTIDE ANTIBIOTICS
URINARY ANTISEPTICS
Nitrofurantoin
Methenamine (Hexamine)
TREATMENT OF URINARY TRACT INFECTIONS
Urinary pH in relation to use of AMAs
Urinary infection in patients with renal impairment
Prophylaxis for urinary tract infection
TREATMENT OF SEXUALLY TRANSMITTED DISEASES (STDs)
CHAPTER 55:
Antitubercular Drugs
NEWER DRUGS
Some antitubercular combinations
Antitubercular combipacks (packs of 1 day's dose)
TREATMENT OF TUBERCULOSIS
SHORT COURSE CHEMOTHERAPY (SCC)
CHAPTER 56:
Antileprotic Drugs
CLASSIFICATION
Dapsone (DDS)
Clofazimine (Clo)
Rifampin (R)
Other antibiotics
TREATMENT OF LEPROSY
Multidrug therapy (MDT) of leprosy
Reactions in leprosy
CHAPTER 57:
Antifungal Drugs
CLASSIFICATION
POLYENE ANTIBIOTICS
Amphotericin B (AMB)
Nystatin
HETEROCYCLIC BENZOFURAN
Griseofulvin
FLUCYTOSINE (5-FC)
IMIDAZOLES AND TRIAZOLES
Ketoconazole (KTZ)
TERBINAFINE
OTHER TOPICAL ANTIFUNGALS
CHAPTER 58:
Antiviral Drugs
CLASSIFICATION
ANTI-HERPES VIRUS DRUGS
Acyclovir
Adverse effects
ANTI-RETROVIRUS DRUGS
Nucleoside reverse transcriptase inhibitors (NRTIs)
Non-nucleoside reverse transcriptase inhibitors (NNRTIs)
Retroviral protease inhibitors (PIs)
FUSION INHIBITOR
Some antiretroviral combinations
HIV TREATMENT GUIDELINES
Prophylaxis of HIV infection
ANTI-INFLUENZA VIRUS DRUGS
Amantadine
Uses
NONSELECTIVE ANTIVIRAL DRUGS
Interferon α
Uses
Adverse effects
CHAPTER 59:
Antimalarial Drugs
CLASSIFICATION
OBJECTIVES AND USE OF ANTIMALARIALS
CHLOROQUINE
Preparations and administration
Uses
MEFLOQUINE
QUININE
Uses
BIGUANIDES
Proguanil (Chloroguanide)
PYRIMETHAMINE
SULFONAMIDE-PYRIMETHAMINE (S/P) COMBINATION
PRIMAQUINE
TETRACYCLINES
ARTEMISININ DERIVATIVES
AMINO-ALCOHOLS
Lumefantrine (see below under ACT)
Artemisinin-based combination therapy (ACT)
CHAPTER 60:
Antiamoebic and Other Antiprotozoal Drugs
ANTIAMOEBIC DRUGS
CLASSIFICATION
METRONIDAZOLE
Preparations
Uses
EMETINE
CHLOROQUINE
AMIDES
Diloxanide furoate
8-HYDROXYQUINOLINES
NOTES ON THE TREATMENT OF AMOEBIASIS
DRUGS FOR GIARDIASIS
DRUGS FOR TRICHOMONIASIS
1. Drugs used orally
2. Drugs used intravaginally
DRUGS FOR LEISHMANIASIS
CHAPTER 61:
Anthelmintic Drugs
SECTION 13: CHEMOTHERAPY OF NEOPLASTIC DISEASES
CHAPTER 62:
Anticancer Drugs
CLASSIFICATION
A. Drugs acting directly on cells (Cytotoxic drugs)
B. Drugs altering hormonal milieu
GENERAL TOXICITY OF CYTOTOXIC DRUGS
NOTES ON INDIVIDUAL DRUGS
ALKYLATING AGENTS
ANTIMETABOLITES
1. Folate antagonist
Methotrexate (Mtx)
2. Purine antagonists
Mercaptopurine (6-MP) and thioguanine (6-TG)
3. Pyrimidine antagonists
VINCA ALKALOIDS
TAXANES
EPIPODOPHYLLOTOXINS
CAMPTOTHECIN ANALOGUES
ANTIBIOTICS
MISCELLANEOUS CYTOTOXIC DRUGS
HORMONES
GENERAL PRINCIPLES IN CHEMOTHERAPY OF CANCER
Toxicity amelioration
SECTION 14: MISCELLANEOUS DRUGS
CHAPTER 63:
Immunosuppressant Drugs, Gene Therapy
IMMUNOSUPPRESSANT DRUGS
Calcineurin inhibitors (Specific T-cell inhibitors)
Antiproliferative drugs(Cytotoxic immunosuppressants)
Glucocorticoids (see Ch. 20)
Immunosuppressant antibodies
Immunosuppression in organ transplantation
GENE THERAPY
APPROACHES IN GENE THERAPY
APPLICATIONS OF GENE THERAPY
CHAPTER 64:
Drugs Acting on Skin and Mucous Membranes
DEMULCENTS
EMOLLIENTS
ADSORBANTS AND PROTECTIVES
ASTRINGENTS
IRRITANTS AND COUNTER-IRRITANTS
CAUSTICS AND ESCHAROTICS
KERATOLYTICS
ANTI-SEBORRHEICS
MELANIZING AGENTS
DRUGS FOR PSORIASIS
DEMELANIZING AGENTS
SUNSCREENS
DRUGS FOR ACNE VULGARIS
1. TOPICAL THERAPY
II. SYSTEMIC THERAPY
TOPICAL STEROIDS
Potent
Moderately potent
Mild
General guidelines for the use of topical steroids
Local adverse effects of topical steroids
Systemic adverse effects of topical steroids
CHAPTER 65:
Antiseptics, Disinfectants and Ectoparasiticides
ANTISEPTICS AND DISINFECTANTS
CLASSIFICATION
1. PHENOLS
2. OXIDIZING AGENTS
3. HALOGENS
4. BIGUANIDE
5. QUATERNARY AMMONIUM (CATIONIC) ANTISEPTICS
6. SOAPS
7. ALCOHOLS
8. ALDEHYDES
9. ACIDS
10. METALLIC SALTS
11. DYES
12. FURAN DERIVATIVES
ECTOPARASITICIDES
CHAPTER 66:
Chelating Agents
CHAPTER 67:
Vitamins
FAT-SOLUBLE VITAMINS
VITAMIN A
Physiological role and actions
Therapeutic uses
Interactions
VITAMIN E
Therapeutic uses
Antioxidant vitamins (vit E, β carotene, vit C) in prevention of cardiovascular disease and cancer
WATER-SOLUBLE VITAMINS
THE VITAMIN B COMPLEX GROUP
Thiamine (Aneurine, vit B1)
Therapeutic uses
Riboflavin (vit B2)
Niacin (vit B3)
Therapeutic uses
Pyridoxine (vit B6)
Drug interactions
Therapeutic uses
Pantothenic acid
Biotin
VITAMIN C (ASCORBIC ACID)
Therapeutic uses
CHAPTER 68:
Vaccines and Sera
VACCINES
BACTERIAL VACCINES
VIRAL VACCINES
TOXOIDS
MIXED ANTIGENS
ANTISERA AND IMMUNEGLOBULINS
CHAPTER 69:
Drug Interactions
MECHANISM OF DRUG INTERACTIONS
Pharmacokinetic interactions
Pharmacodynamic interactions
Drug interactions before administration
Selected References for Further Reading
APPENDICES
APPENDIX - 1:
List of Essential Medicines
A
B
C
D
E
F
G
H
I
K
L
M
N
O
P
Q
R
S
T
U
V
W
X
Z
APPENDIX - 2:
Prescribing in Pregnancy
APPENDIX - 3:
Drugs in Breastfeeding
APPENDIX - 4:
Drugs and Fixed Dose Combinations Banned in India
INDEX
TOC
Index
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