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Illustrated Medical Pharmacology
SM Raju, AK Kapoor
SECTION 1: GENERAL PHARMACOLOGY
CHAPTER 1.1:
Introduction and Terminology
TERMINOLOGY
Pharmacokinetics
Pharmacodynamics
Pharmacotherapeutics
Clinical Pharmacology
Chemotherapy
Toxicology
Pharmacy
Pharmacopeia
Pharmaceutics
NOMENCLATURE OF DRUGS
SOURCES OF DRUGS
Products from Natural Sources
Synthetic Products
Products of Genetic Engineering
Prodrugs
FACTORS AFFECTING DOSAGE AND THERAPEUTIC RESPONSE
Factors to Consider while Calculating the Therapeutic Dose
EFFECTS OF DRUG INTERACTIONS
Secondary Effects
Drug-food Interactions
Drug-drug Interaction
Placebo Effect
Drug Dependency
Tolerance
Cross-tolerance
Tachyphylaxis
DRUG THERAPY MONITORING
LEGISLATION REGARDING NARCOTIC DRUGS
DRUG DOSAGE CALCULATIONS
Formulae for Calculating Doses for Children
Young Formula
Square Meter Surface Area Method
Clark's Formula
BIOTRANSPORTATION OF DRUGS
Passive Diffusion
Carrier-Mediated Transport
Filtration
Pinocytosis
DRUG ABSORPTION
Functional Groups Involved in Drug Absorption
Ionizable Groups on a Drug Molecule Alter their Absorption and Excretion
P-glycoprotein Expression Modulates Drug Absorption and Distribution
DRUG ABSORPTION
Methods of Delaying Drug Absorption
Methods to Facilitate Absorption
First Pass Effect Alters the Bioavailability of Drugs
DRUG DISTRIBUTION
Physiological Barriers of Drug Distribution
Blood-brain Barrier
Placental Barrier
DRUG METABOLISM
Drug Transformation Reactions
Phase I Reactions
Phase II Reactions
Other Drug Interactions that Influence Drug Metabolism
PEDIATRIC PHARMACOLOGY
GERIATRIC PHARMACOLOGY
PHARMACOGENETICS
Anticancer Drugs and Pharmacogenomics (Fig. 1.1.13)
OTHER EXAMPLES OF GENETIC MUTATIONS AFFECTING DRUG RESPONSES
Vampire Syndrome
Hereditary Methemoglobinemia
PEDIATRIC (NEONATE TO ABOUT 16 YEARS)
GERIATRIC (AGED ABOVE 65 YEARS)
WOMEN
Introduction to Drug Action
Disease Classification
Drug Classification
Drug Names
Mode of Drug Action
Killing Foreign Organisms
Stimulation and Depression
Sites of Drug Action
ENZYME INHIBITION
Mechanisms of Drug Actions by Enzyme Inhibition
DRUG RECEPTOR INTERACTIONS
Drug Interaction with Receptor Site
Drug Development and Approval Process
CHAPTER 1.2:
Routes of Drug Administration
ENTERAL ROUTE
Oral Route
Local Treatment
General Treatment
Drug Absorption
Mechanism of Drug Absorption
Factors Modifying Gastrointestinal Absorption and Bioavailability
Form or Presentation of the Drug
Foods
Total Surface Area Available
Solubility of Drug
Chemical Instability
Transit in the Digestive Tract
Drug Interaction in the Digestive Tract
Gastrointestinal Tract Diseases
PARENTERAL ROUTE
Various Parenteral Routes
Intradermal Route
Subcutaneous Route
Intramuscular Route
Intravenous Route
Intra-arterial Route
Intracardiac Injection
Factors Modifying Parenteral Absorption of Drugs
Dosage Form
Physical Characteristics of the Drug
Application of Tourniquet
Addition of Vasoconstrictor Drugs
Rate of Diffusion Through Tissues
Temperature at the Site of Injection
Method of Giving the Intramuscular Injection
Choosing the Site for Intramuscular Injection
Giving Subcutaneous Injections
Giving Intravenous Injection
NASAL ROUTE
CUTANEOUS OR TRANSDERMAL ROUTE
TOPICAL (LOCAL) ROUTE
Transdermal Adhesive Patches
Inunctions (Rubbing)
Vaginal and Urethral Applications
Application of Drugs to the Vagina and Uterus
OTHER ROUTES
Pulmonary Route (Inhalation)
Local Treatment
General Treatment
Ocular, Ear and Vaginal Routes
PARTICULAR PREPARATIONS
Liposomes
Virus Vectors
BIOAVAILABILITY
BIOEQUIVALANCE
CHAPTER 1.3:
Pharmacokinetics and Pharmacodynamics
PHARMACOKINETICS
Basic Processes in Pharmacokinetics
Step 1: Drug Absorption
Step 2: Drug Distribution
Step 3: Drug Metabolism
Step 4: Drug Elimination
Pharmacokinetic Definitions
Area-Under-the-Curve
Maximum Concentration (Cmax)
Minimum Concentration (Cmin or Trough)
Half-life (t ½)
Steady-state
Adherence
Clinical Pharmacokinetics
First Order Elimination Kinetics
Zero Order Elimination Kinetics
Drugs with Dose-dependent Kinetics of Elimination
PHARMACODYNAMICS
Effects on the Body
Desired Activity
Undesirable Effects
Therapeutic Window
Receptor Binding
Volume of Distribution
Clinical Pharmacodynamics
REVIEW QUESTIONS
CHAPTER 1.4:
Biotransformation of Drugs
DRUG METABOLISM
Major Enzymes and Pathways
Phase I Reactions
Summary of Phase I Reactions
Phase II Reactions
Summary of Phase II Reactions
Phase III Reactions
Phase IV Reactions
Sites of Drug Metabolism
Factors Affecting Drug Metabolism
SECTION 2: DRUGS AFFECTING AUTONOMIC NERVOUS SYSTEM
CHAPTER 2.1:
Autonomic Nervous Systems
NERVOUS SYSTEMS
Central Nervous System
Peripheral Nervous System
Afferent Division
Efferent Division
NEUROTRANSMITTERS
Neurotransmitters of Autonomic Nervous System
Why are There so Many Brain Neurotransmitters?
Acetylcholine
CHOLINERGIC RECEPTORS
Muscarinic Receptors
M1 Receptors
M2 Receptors
M3 Receptors
Nicotinic Receptors
Nicotinic 1 (N1) Receptors
EFFECTS OF DRUGS
Excitant or Stimulant Effects of a Drug
Depressant or Inhibitory Effects of Drug
Causes of Untoward Effects of Drugs
REVIEW QUESTIONS
CHAPTER 2.2:
Adrenergic Drugs
ADRENERGIC RECEPTORS
Mechanism of Adrenergic Receptors
Adrenergic Neurotransmissions
Types of Adrenergic Receptors
Alpha Receptor
Beta Receptor
Desensitization of Receptors
ADRENERGIC STIMULANTS (AGONISTS)
Clinical Uses
Anaphylactic Shock
Cardiac Activation
Bronchodilators
Nasal Decongestants and Vasopressors
In Combination with Local Anesthetics
Glaucoma
Direct-acting Adrenergic Agonists
Norepinephrine (Levophed)
Epinephrine
Dopamine (Intropin)
Dobutamine (Dobutrex)
Dopexamine
Isoproterenol (Isuprel)
β2-selective Adrenergic Agonists
α1-selective Adrenergic Agonists
α2-selective Adrenergic Agonists
Indirectly Acting Sympathomimetic Agents
Amphetamine
Tyramine
Cocaine
Mephentermine (Wyamine)
Mixed Action Adrenergic Agonists
Ephedrine and Pseudoephedrine
Metaraminol (Aramine)
SUMMARY OF CLINICAL USES OF SYMPATHOMIMETIC AGENTS
Nonselective Adrenergic Agonists
α1-selective Agonists
α2-selective Agonists
β1-adrenergic Receptor Selective Agonists
β2-selective Agonists (various drugs)
ADRENERGIC ANTAGONISTS (BLOCKERS)
α1-adrenergic Receptor Antagonists
α2-adrenergic Receptor Antagonists
Clinical Uses of α-adrenergic Antagonist Drugs
Phenoxybenzamine (Dibenzyline)
Phentolamine (Regitine) and Tolazoline (Priscoline)
Prazosin (Minipress) and Terazosin (Hytrin)
Yohimbine
β-adrenergic Antagonists
Pharmacologic Effects of β-adrenergic Antagonists
Non-selective β-adrenergic Receptor Antagonists
Selective β1-adrenergic Receptor Antagonists
β-blockers with Partial Agonist Activity
Use in Hypertension
Therapeutic Uses of β-adrenoceptor Antagonists
Untoward Effects of β-adrenoceptor Antagonists
Drug Interactions
DRUGS AFFECTING NEUROTRANSMITTER RELEASE OR UPTAKE
Reserpine
Guanethidine
Cocaine
CONDITIONS THAT RESEMBLE MYASTHENIA GRAVIS
Neurasthenia
Associated Disorders
REVIEW QUESTIONS
CHAPTER 2.3:
Cholinergic Drugs
CELLULAR EVENTS FOLLOWING CHOLINERGIC RECEPTOR ACTIVATION
Nicotinic Muscle Receptor
Nicotinic Neuronal Receptor
Muscarinic Type M1
Muscarinic Type M2
Atrium
Atrioventricular Node
Ventricle
SECOND MESSENGER SYSTEMS
Muscarinic Receptor Activation by Nitric Oxide
Nitric Oxide Synthase
STIMULATION OF CHOLINERGIC RECEPTORS
Direct Acting Cholinergic Agonists
Cholinergic Agonist Drugs
Cholinergic Poison Agents
Indirect Acting Cholinergic Agents
Physostigmine
Neostigmine
Pyridostigmine
Clinical Uses of Cholinergic Agonists
Gastrointestinal and Genitourinary
Ophthalmologic Uses
Adverse Effects of Muscarinic Agonists
Major Contraindication to the Use of Muscarinic Agonists (Choline Esters)
Pharmacokinetics of Acetylcholinesterase Inhibitors
Organophosphate Insecticides
Organophosphates (Example: Di-isopropyl Fluorophosphate)
Organophosphorus Warfare Nerve Agents
Carbamates (e.g. Physostigmine and Neostigmine)
Parathion
Malathion
Echothiophate
Clinical Uses
Antidote for Organophosphates
Pralidoxime
Atropine
ANTAGONISTS (INHIBITION) OF CHOLINERGIC RECEPTORS
Clinical Uses of Cholinergic Receptor Blockers
Scopolamine
Atropine
Botulinum Toxin
Botox
Antispasmodics
Smooth Muscle Spasm
REVIEW QUESTIONS
CHAPTER 2.4:
Antimyasthenic Drugs
CLASSIFICATION OF ANTIMYASTHENIC DRUGS
Acetylcholinesterase Inhibitors
Neostigmine (Prostigmin, Vagostigmin)
Pyridostigmine (Mestinon)
Edrophonium
Immunosuppressive Drugs
Azathioprine (Imuran)
Drugs which Aggravate Myasthenia Gravis
REVIEW QUESTIONS
SECTION 3: DRUGS AFFECTING CENTRAL NERVOUS SYSTEM
CHAPTER 3.1:
Central Nervous System
NEUROTRANSMITTERS
Norepinephrine
Serotonin
Dopamine
Acetylcholine
CENTRAL NERVOUS SYSTEM STIMULANTS
Caffeine
Amphetamines
ANTIDEPRESSANT
Tricyclic Antidepressants
Imipramine (Tofranil) and Desipramine (Norpramin)
Inhibitory Action of Antidepressants on Serotonin Uptake
Selective Serotonin Reuptake Inhibitors
Monoamine Oxidase Inhibitors
HALLUCINOGENIC DRUGS
Mescaline and Psilocybin
Lysergic Acid Diethylamide
CENTRAL NERVOUS SYSTEM DEPRESSANTS—SEDATIVE AND HYPNOTIC AGENTS
Barbiturates
Benzodiazepines
NARCOTIC ANALGESIC DRUGS
Receptor Site
Natural Peptide Analgesics
Enkephalins
Morphine and Codeine
Heroin
Synthetic Narcotic Analgesics
Meperidine
Methadone
NARCOTIC ANTAGONISTS
LOCAL ANESTHETICS
REVIEW QUESTIONS
CHAPTER 3.2:
Anxiolytics and Sedative–Hypnotics
CLASSIFICATION OF ANXIOLYTICS AND HYPNOTIC DRUGS
PHARMACOKINETICS
Mechanism of Action of Anxiolytics, Sedatives and Hypnotics
Benzodiazepines
Pharmacological Effects
Barbiturates
Pharmacological Effects
Advantages and Disadvantages of Benzodiazepines versus Barbiturates
Ethanol
Metabolism
Drug-drug Interactions
Contraindications
Disulfiram
Major Anxiolytic Drug Classes
Buspirone
MAJOR HYPNOTIC DRUG CLASSES
Benzodiazepines
Barbiturates and Non-barbiturates Hypnotics
Untoward Effects
Management of Barbiturate Poisoning
Therapeutic Uses
Specific Hypnotics
Clonazepam
Flurazepam (Dalmane)
Triazolam (Halcion)
BENZODIAZEPINE ANTAGONIST
Flumazenil (Romazicon)
Untoward Effects
Drug Interactions
REVIEW QUESTIONS
CHAPTER 3.3:
Antiepileptics
EPILEPSY
ANTIEPILEPTIC AGENTS
Phenytoin (Dilantin)
Carbamazepine (Tegretol)
Phenobarbital (Solfoton)
Primidone (Mysoline)
Ethosuximide (Zarontin)
Valproate (Depakene)
Gabapentin (Neurontin)
Diazepam (Valium)
Lorazepam (Ativan)
Benzodiazepine
Lamotrigine (Lamictal)
Tiagabine (Gabitril)
Topiramate (Topamax)
Zonisamide (Zonegran)
SPECIAL CONSIDERATIONS FOR STARTING ANTIEPILEPTIC THERAPY
REVIEW QUESTIONS
CHAPTER 3.4:
General Anesthetics
CLASSIFICATION OF DRUGS USED FOR GENERAL ANESTHESIA
PROCEDURE FOR GENERAL ANESTHESIA
Preanesthetic Evaluation
Patient's Factors in Selection of Anesthesia
Premedication
Administration of General Anesthesia
Inhalation Anesthetics
Mechanism of Action of Inhaled Anesthetics
Intravenous Anesthetics
Monitoring
Airway Management
Postoperative Care (Pain Relief)
STAGES OF ANESTHESIA
Induction
Depth of Anesthesia (Stages of Induction)
Maintenance
Recovery
Muscle Relaxation/Neuromuscular Blockade
CAUSES OF MORTALITY
INTRAVENOUS ANESTHETICS
Ketamine
Mode of Action
Pharmacokinetics
Clinical Use
Dosage
Contraindications
Precautions
Drug Interactions
Untoward Effects
Drug Toxicity
Thiopentone Sodium
Mode of Action
Pharmacokinetics
Clinical Use
Dosage
Contraindications
Precaution
Drug Interactions
Untoward Effects
Toxicity and its Treatment
Propofol
Opioids
INHALATION ANESTHETICS
Halothane
Mode of Action
Pharmacokinetics
Clinical Use
Dosage
Routes of Administration
Contraindications
Precaution
Drug Interactions
Untoward Effects
Toxicity
Isoflurane
Mode of Action
Pharmacokinetics
Clinical Use
Dosage
Routes of Administration
Contraindications
Precaution
Drug Interactions
Untoward Effects
Toxicity
Desflurane
Nitrous Oxide
REVIEW QUESTIONS
CHAPTER 3.5:
Local Anesthetics
CLASSIFICATION OF LOCAL ANESTHETICS
Natural Local Anesthetics
Synthetic Local Anesthetics
PROPERTIES
MECHANISM OF ACTION OF LOCAL ANESTHETICS
PHARMACOKINETICS
Absorption and Distribution
Metabolism and Excretion
EFFECTS OF LOCAL ANESTHETICS
Effects on Fetus when Given in Pregnancy
Effects of Addition of Adrenaline, Felypressin, Bicarbonate and Glucose on the Action of Local Anesthetics
Adrenaline
Felypressin
Bicarbonate
Glucose
Factors Affecting the Local Anesthetic Effects
Ionization
Vasodilation
Lipid Solubility
Vascularity
Vasoconstrictors
Plasma Concentration
Placental Transfer
Combinations of Local Anesthetic
Disadvantage
Untoward Effects of Local Anesthetic
Systemic Toxicity
Allergic Reaction
Cross Sensitivity
Toxicity to Central Nervous System
Neurotoxicity
Cauda Equina Syndrome
PREPARATIONS
CLINICAL USES OF LOCAL ANESTHETICS
Regional Anesthesia
Topical (Surface) Anesthesia
Local Infiltration
Peripheral Nerve Block
Mechanism
Intravenous Regional Anesthesia (Bier Block)
Epidural Anesthesia
Spinal Anesthesia
Cocaine Toxicity
Untoward Effects of Acute Administration
Treatment of Cocaine Toxicity
REVIEW QUESTIONS
CHAPTER 3.6:
Parkinson's Disease
CLINICAL MANIFESTATIONS
MEDICATIONS FOR PARKINSON'S DISEASE
Levodopa (Dopar)
Pharmacokinetics
Clinical Use
Untoward Effects
Drug Interactions
Contraindications
Carbidopa (Lodosyn)
Dopamine Agonists
Bromocriptine (Parlodel)
Pergolide (Permax)
Pramipexole
Ropinirole
Untoward Effects of Dopamine Agonists
Monoamine Oxidase Inhibitors
Selegiline or Deprenyl (Eldepryl)
Rasagiline
Anticholinergic (Antimuscarinic) Drugs
Benztropine (Cogentin)
Other Drugs
Amantadine (Symmetrel)
REVIEW QUESTIONS
CHAPTER 3.7:
Skeletal Muscle Relaxants
SPASTICITY
Clinical Spasticity
SPASMOLYTIC AGENTS
Clinical Use
Mechanism of Action
Diazepam (Valium)
Baclofen (Lioresal)
Tizanidine (Zanaflex)
Dantrolene (Dantrium)
Botulinum Toxin-A (BOTOX)
Mechanism of Action
Clinical Uses
Gabapentin
Glycine
Idrocilamide
Commonly Used Drugs for Acute Local Spasm
NEUROMUSCULAR BLOCKING AGENTS
Classification of Neuromuscular Blocking Drugs
Non-depolarizing (Competitive) Blocking Agents
Depolarizing Blocking Agents
Mechanism of Action of Neuromuscular Blocking Agents
Mechanism of Non-depolarizing Blocking Agents
Mechanism of Depolarizing Blocking Agents
Pharmacokinetics
Pharmacodynamics
Clinical Uses
Why Monitor Neuromuscular Blockade?
Untoward Effects
NON-DEPOLARIZING NEUROMUSCULAR BLOCKING AGENTS
Major Classes of Non-depolarizing Blocking Drugs
Long Acting Non-depolarizing Blockers
Doxacurium (Nuromax)
Pancuronium (Pavulon)
Pipecuronium (Arduan)
Intermediate-acting Non-depolarizing Blockers
Atracurium (Tracrium)
Cisatracurium (Nimbex)
Vecuronium (Norcuron)
Special Considerations
Rocuronium (Zemuron)
Effects on Muscle Groups
Pharmacokinetics
Cardiovascular Effects
Short-acting Non-depolarizing Neuromuscular Blocker
Mivacurium (Mivacron)
DEPOLARIZING NEUROMUSCULAR BLOCKING DRUGS
Succinylcholine (Anectine)
Mechanism of Action
Duration of Action
Untoward Effects
SKELETAL MUSCLE SPASM
Cyclobenzaprine (Flexeril and Fexmid)
Mechanism of Action
Clinical Uses
Recreational Use
Formulations and Dosages
Untoward Effects
Drug Interactions
Carisoprodol (Carisoma, Sanoma)
Pharmacokinetics
Pharmacological Effects
Clinical Uses
Untoward Effects
Orphenadrine (Norflex, Mephenamin)
Pharmacological Effects
Clinical Uses
Dosage and Delivery
Untoward Effects
Drug Interactions
CLINICAL PHARMACOLOGY OF NEUROMUSCULAR-BLOCKING AGENTS
Dose Guidelines
REVERSAL OF NEUROMUSCULAR BLOCKADE BY ANTAGONIST
Special Considerations in Reversal of Neuromuscular Blockade
Use of Muscarinic Antagonists with Anticholinesterases
Factors Influencing the Reversal of Neuromuscular Blockade by Anticholinesterase Agents
Neuromuscular Blockade by Succinylcholine followed by Non-depolarizing Agent
Combinations of Neuromuscular-blocking Agents
Gender and Neuromuscular Blockade
REVIEW QUESTIONS
CHAPTER 3.8:
Antipsychotic Drugs
SCHIZOPHRENIA
CLASSIFICATION OF ANTIPSYCHOTIC DRUGS (TABLE 3.8.1)
CLINICAL USES OF ANTIPSYCHOTICS
Phenothiazine Compounds
Chlorpromazine (Thorazine)
Butyrophenones
Haloperidol (Haldol)
Miscellaneous/Atypical Antipsychotics
Risperidone (Risperdal) (Fig. 3.8.6)
Clozapine (Clozaril)
Olanzapine (Zyprexa)
Effects of Antipsychotic Agents on Prolactin
ANTIMANIC AGENTS
Lithium
Pharmacokinetics
Possible Mechanisms of Action
Clinical Uses
Drug-Drug Interactions
Contraindication
Untoward Effects
Lithium and Pregnancy
REVIEW QUESTIONS
CHAPTER 3.9:
Central Nervous System Stimulants and Antidepressants
STIMULANTS OF CENTRAL NERVOUS SYSTEM
Cortical Stimulants
Psychomimetics
Mechanism of Action
Untoward Effects (Toxic Effects)
Clinical Uses
Cocaine HCl
Methylxanthines (Theophylline, Caffeine and Theobromine)
Nootropic Drugs
Brainstem Stimulants
Picrotoxin
Pentylenetetrazole
Doxapram
Spinal Cord Stimulants
Strychnine
Serotonin Pharmacology
Sumatriptan (Imitrex)
SEROTONIN ANTAGONISTS
Cyproheptadine (Periactin)
Clinical Use
Ketanserin
Ritanserin
Ondansetron (Zofran)
Tropisetron
Clinical Use
Granisetron (Kytril)
Clinical Use
Dolasetron
Clinical Use
ANTIDEPRESSANT AGENTS
Unipolar Depression
Criteria for Diagnosis of Unipolar Depression (Major Depression)
Bipolar Depression
Criteria for Diagnosis of Bipolar Depression (Mania)
Antidepressant: Classification
Tricyclic Antidepressants
Monoamine Oxidase Inhibitors
Second Generation Drugs (not Including SSRIs)
Serotonin Selective Reuptake Inhibitors
Withdrawal Effects
Fluoxetine (Prozac)
Clinical Uses
Adverse Effects
Drug Interactions
Untoward Effects of Other Antidepressants
REVIEW QUESTIONS
CHAPTER 3.10:
Opioid Analgesic and Antagonists
DISTRIBUTION OF OPIOID RECEPTORS AND THEIR INFLUENCE
CLASSIFICATION OF OPIOIDS (TABLE 3.10.1)
EFFECT OF OPIOID ANALGESICS ON THE CENTRAL NERVOUS SYSTEM
Morphine
Opioid and Analgesic Combinations
Antitussives
Chemical Modifications
Endogenous Opioid Peptides
PHARMACOKINETICS
PHARMACODYNAMICS
NEUROCHEMISTRY OF PAIN
Abuse of Opioid
Tolerance/Physical Dependence
ORGAN SYSTEM EFFECTS OF OPIOIDS
Central Nervous System Effects
Spinal Cord Sites of Action
Supraspinal Sites of Action
Euphoria
Sedation
Respiratory Depression
Cough Suppression
Miosis (Pupillary Constriction)
Truncal Rigidity
Nausea and Vomiting
Cardiovascular Effects
Gastrointestinal Effects
Biliary Tract
Urinary Tract
Neuroendocrine Effects
Other Effects
ORGAN SYSTEM EFFECTS OF PENTAZOCINE AND OTHER AGONIST-ANTAGONISTS
Toxic Effects of Opioids
Nausea and Vomiting
Untoward Effects
Tolerance
Cross-tolerance
Physiologic Dependence
Antagonist-precipitated Withdrawal
Psychological Dependence
CLINICAL USES
Pain Management
Obstetrical Labor
Renal/Biliary Colic
Acute Pulmonary Edema
Cough
Diarrhea
Opioids and Anesthesia
Intraoperative Use (General)
Intraoperative Use (Regional)
Other Routes of Administration
Prescribing Principles and Guidelines
Management of Opioid Overdosage
Pregnancy
Patients with Impaired Lung Function
Patients with Impaired Hepatic or Renal Function
Patients with Endocrine Disorders
SPECIFIC DRUGS
Strong Agonists
Methadone (Dolophine)
Levomethadyl Acetate (L-acetylmethadol)
Meperidine (Demerol)
Fentanyl Group
Morphinans
Mild/Moderate Agonists
Phenanthrenes
Phenylheptylamines
Phenylpiperidines
Mixed Agonist-Antagonists and Partial Agonists
Phenanthrenes
Morphinans
Benzomorphans
Miscellaneous
Antitussives
OPIOID ANTAGONISTS (PURE ANTAGONISTS)
Pharmacodynamics of Opioid Antagonists
Antagonist Drugs
Naloxone
Naltrexone
Nalmefene
REVIEW QUESTIONS
CHAPTER 3.11:
Ergot Alkaloids
CLASSIFICATION
ORGAN SYSTEMS EFFECTED BY ERGOT ALKALOIDS
Central Nervous System
Vascular Smooth Muscle
Uterine Smooth Muscle
Other Smooth Muscle
MIGRAINE
Drug Treatment for Migraine
Migraine Prophylaxis
Propranolol (Inderal) or Timolol (Blocadren)
Ergonovine and Methysergide (Sansert)
Amitriptyline (Elavil)
Cyproheptadine
Verapamil
Caffeine (Methylxanthines)
Sumatriptan (Imitrex)
Ergotamine (Cafergot, Ergomar)
Morphine or Hydromorphone (Dilaudid)
Other Drugs Used
Management of Nausea
Metoclopramide (Reglan)
Diphenhydramine and Dimenhydrinate
Untoward Effects of Drugs used in Migraine
Therapy of Hyperprolactinemia
Therapy of Postpartum Hemorrhage
REVIEW QUESTIONS
CHAPTER 3.12:
Alcohols
IMPORTANT COMMONLY ENCOUNTERED ALCOHOLS
Methyl Alcohol
Isopropyl Alcohol
Ethyl Alcohol
EFFECTS OF ALCOHOL
Effect on Central Nervous System
Concentration Response
Cardiovascular Effects
Gastrointestinal Effects
Effects on Liver
Effects on Kidney
Impotence
Other Effects of Alcohol
PHARMACOKINETICS
ALCOHOL ABUSE
Chronic Use (Alcohol Tolerance and Physical Dependence)
Neuropathic Changes
Alcohol Withdrawal
Treatment
Pharmacological Treatment
METHANOL ABUSE
Treatment
CHAPTER 3.13:
Drug Abuse
MEDICAL DEFINITIONS
SIGNS AND SYMPTOMS
DRUG ABUSE
Prescription Drug Abuse
Pain Relievers
Addictive Drugs of Abuse
Biochemical Mechanism of Addiction
Dependence and Tolerance
Non-addictive Drugs of Abuse
Treatment
SECTION 4: DRUGS ACTING ON CARDIOVASCULAR AND RENAL SYSTEM
CHAPTER 4.1:
Antihyperlipidemic Agents
LIPOPROTEIN METABOLISM
STRATEGIES FOR TREATING HYPERLIPIDEMIAS
First Line of Agents
Statins
Bile Acid Sequestering Agents
Ezetimibe
Second Line of Agents
Fibrates
Nicotinic Acid
REVIEW QUESTIONS
CHAPTER 4.2:
Anticoagulants
ANTICOAGULANT DRUGS
Types of Anticoagulant Drugs
CLASSIFICATION OF ANTICOAGULANTS
Parenteral Anticoagulants
Heparin and Low-molecular Weight Heparin
Heparin Antagonists
Oral Anticoagulants
Warfarin Antagonists
CLINICAL USES OF ANTICOAGULANTS
RECOMMENDED DOSAGE
PRECAUTIONS
UNTOWARD EFFECTS
INTERACTIONS
CHAPTER 4.3:
Thrombolytic Drugs
THROMBOLYTIC THERAPY
Description
Recommended Dosage
Precautions
Untoward Effects
Interactions
Fibrin Clot Formation
Tissue Plasminogen Activators
Recombinant Tissue Plasminogen Activator (Alteplase)
Streptokinase
Urokinase
Adverse Effects and Contraindications
CHAPTER 4.4:
Antiplatelet Drugs
ASPIRIN
Dose and Duration
Adverse Effects
THIENOPYRIDINES
Clopidogrel
Clinical Uses
Adverse Effects
Ticlopidine
Mechanism of Action
Contraindications
Precautions
GLYCOPROTEIN IIB/IIIA RECEPTOR ANTAGONISTS
OTHER ANTIPLATELET DRUGS
CHAPTER 4.5:
Antiarrhythmic Drugs
THERAPEUTIC USE
MECHANISM OF ACTION
Treatment of Arrhythmias
CLASSES OF DRUGS USED TO TREAT ARRHYTHMIAS
Sodium-channel Blockers (Class I)
General Pharmacology
Effects on Depolarization
Effects on Repolarization
Effects on Automaticity
Indirect Vagal Effects
Specific Drugs and Therapeutic Indications
Quinidine (Quinidex)
Lidocaine
Flecainide
Side Effects and Contraindications
β-blockers (Class II Antiarrhythmics)
Potassium-channel Blockers (Class III Antiarrhythmics)
Specific Drugs and Therapeutic Indications
Side Effects and Contraindications
Calcium-channel Blockers (Class IV)
Therapeutic Use of Calcium-channel Blockers
Different Classes of Calcium-channel Blockers
Side Effects and Contraindications
Miscellaneous
Adenosine
Therapeutic Use and Rationale
Side Effects and Contraindications
REVIEW QUESTIONS
CHAPTER 4.6:
Vasoactive Drugs
VASODILATORS
Arterial Dilators
Venous Dilators
Mixed or Balanced Dilators
Untoward Effects of Vasodilators
Clinical Use
Nitroprusside Sodium and Diazoxide
Hydralazine and Minoxidil
Vasodilator Drug Classes
Calcium-channel Blockers
Amlodipine and Felodipine
Untoward Effects
Nimodipine
Angiotensin Converting Enzyme Inhibitor
Captopril
Angiotensin Receptor Blocker
PRESSOR DRUGS
VASOCONSTRICTORS
Constriction of Arterial (Resistance) Vessels
Constriction of Venous (Capacitance) Vessels
Drug Classes, General Mechanisms of Action, and Contraindications
α-adrenoceptor Agonists (α-agonists)
Specific Drugs and Therapeutic Uses
Side Effects and Contraindications
Vasopressin Analogs
Side Effects and Contraindications
REVIEW QUESTIONS
CHAPTER 4.7:
Cardioinhibitory Drugs
THERAPEUTIC USES OF CARDIOINHIBITORY DRUGS
Hypertension
Angina and Myocardial Infarction
Arrhythmias
Heart Failure
DRUG CLASSES AND GENERAL MECHANISMS OF ACTION
Beta-blockers
Therapeutic Uses
Different Classes of Beta-blockers and Specific Drugs
Side Effects and Contraindications
Centrally Acting Sympatholytics
Heart
Blood Vessels
Calcium-channel Blockers
Therapeutic Use
Different Classes
Untoward Effects and Contraindications
CHAPTER 4.8:
Cardiostimulatory Drugs
THERAPEUTIC USE OF CARDIOSTIMULATORY DRUGS
Heart Failure and Cardiogenic Shock
Circulatory Shock
DRUG CLASSES AND GENERAL MECHANISMS OF ACTION
Beta-agonists
Digitalis Compounds
Phosphodiesterase Inhibitors
Calcium-sensitizing Drugs
CHAPTER 4.9:
Diuretics
FORMATION OF URINE
THERAPEUTIC USES
Cardiovascular Effects of Diuretics
Hypertension
Angiotensin Converting Enzyme Inhibitors (ACE Inhibitors)
Heart Failure
Pulmonary and Systemic Edema
TYPES OF DIURETICS
Carbonic Anhydrase Inhibitors
Acetazolamide (Generic, Diamox)
Thiazide Diuretics
Chlorothiazide (Generic, Diuril)
Hydrochlorothiazide (Generic, Microzide)
Indapamide (Generic, Lozol)
Loop (High-ceiling) Diuretics
Furosemide (Generic, Lasix)
Ethacrynic Acid (Edecrin)
Torsemide (Demadex)
Potassium-sparing Diuretics
Triamterene (Dyrenium)
Amiloride (Midamor)
Spironolactone (Generic, Aldactone)
Eplerenone (Inspra)
Osmotic Diuretics
REVIEW QUESTIONS
CHAPTER 4.10:
Antihypertensive Drugs
HYPERTENSION
RATIONALE OF REDUCING ARTERIAL PRESSURE
Reduce Cardiac Output
Reduce Systemic Vascular Resistance
ANTIHYPERTENSIVE DRUGS
Diuretics
Chlorothiazide (Diuril)
Loop Diuretics
Untoward Effects
SYMPATHOLYTICS
Centrally Acting Sympatholytic
Clonidine
Methyldopa
Adrenergic Neuron Blocker
Guanethidine
Reserpine
Adrenoceptor Antagonists
Beta Blockers
Labetalol
Prazosin and Terazosin Doxazosin
ANGIOTENSIN CONVERTING ENZYME INHIBITORS
Angiotensin II Receptor Antagonists
REVIEW QUESTIONS
CHAPTER 4.11:
Antianginal Drugs
ANGINA
Types of Angina
Variant Angina (Prinzmetal's)
Chronic Stable Angina
Unstable Angina
Therapeutic Use and Rationale
Classes of Drugs Used in the Treatment of Angina
NITRATES
Mechanism of Action
Pharmacological Actions
Pharmacokinetics
Clinical Uses
Angina Pectoris
Congestive Heart Failure and Acute Left Ventricular Failure
Myocardial Infarction
Interventional Cardiac Procedures
Biliary Colic
Esophageal Spasm
Cyanide Poisoning
Specific Drugs
Nitroglycerin
Isosorbide Dinitrate and Mononitrate
Sodium Nitroprusside
Untoward Effects and Contraindications
β-BLOCKERS
Mechanism of Action
Phenylalkylamines
Verapamil
Benzothiazepines
Diltiazem
Dihydropyridines
Nifedipine
Amlodipine
Untoward Effects
Beneficial Combinations in Angina
POTASSIUM-CHANNEL OPENERS
Types of Potassium-Channels
Voltage-gated K+ Channels
Calcium Activated K+ Channels
ATP Sensitive K+ Channels
Nicorandil
Untoward Effects
Role of each Drug used in the Treatment of Angina
MYOCARDIAL INFARCTION
Management of Myocardial Infarction
Thrombolytic Therapy
Contraindications
Post-thrombolytic Management
Action of IV Morphine in MI
REVIEW QUESTIONS
CHAPTER 4.12:
Cardiac Glycosides
MECHANISM OF ACTION
PHARMACOLOGICAL ACTIONS
Cardiac Effects
Extracardiac Effects
Diuretic Effect
Autonomic Nervous System Effect
Central Nervous System Effect
Vascular Effect
Gastrointestinal Effects
TOXICITY OF DIGITALIS
CONTRAINDICATIONS TO DIGITALIS THERAPY
DRUG INTERACTIONS
CLINICAL USES
OUABAIN
REVIEW QUESTIONS
SECTION 5: ENDOCRINE DRUGS
CHAPTER 5.1:
Hypothalamic and Pituitary Hormones
HYPOTHALAMUS
PITUITARY GLAND
Anterior Pituitary (Adenohypophysis)
Posterior Pituitary (Neurohypophysis)
Intermediate Lobe
PITUITARY HORMONES
Tropic Hormone
Non-tropic Hormone
Functions of Pituitary Hormones
Feedback Relationships
Pituitary Control
Pituitary Secretion Control
Mechanism of Action of Corticotropin-releasing Hormone
Physiological Consequences of Pituitary Tumors
Hypothalamic Disease
Mechanisms of Action of Peptide Hormone
Growth Hormone/Somatotropin
Pharmacokinetics
Mechanism of Action
Clinical Uses
Pharmacological Effects
Untoward Effects of GH Therapy
Contraindications
Somatostatin
Thyrotropin-releasing Hormone (Protirelin)
Pharmacokinetics
Pharmacodynamics
Thyrotropin-releasing Hormone Infusion Test
Thyroid-stimulating Hormone (Thyrotropin)
Pharmacokinetics
Pharmacodynamics
Clinical Use
Corticotropin-releasing Hormone
Pharmacokinetics
Pharmacodynamics
Adrenocorticotropic Hormone (Corticotropin)
Pharmacokinetics
Pharmacodynamics
Mechanism of Action
Clinical Uses
Adverse Effects
Gonadotropin-releasing Hormone (Luteinizing Hormone-releasing Hormone, Gonadorelin)
Pharmacokinetics
Pharmacodynamics
Clinical Uses
Toxicity
Contraindications
Follicle-stimulating Hormone
Physiological Functions
Modified FSH Molecules
Luteinizing Hormone
Physiological Functions
Human Menopausal Gonadotropins (Menotropins and Urofollitropin)
Pharmacokinetics
Pharmacodynamics
Clinical Uses
Untoward Effects
Contraindications
Hypothalamic and Pituitary Agents
Human Chorionic Gonadotropin
Pharmacokinetics
Pharmacodynamics
Clinical Uses
Therapeutic Application
Untoward Effects
Contraindication
Prolactin
Physiological Effects
Bromocriptine and Other Dopamine Agonists
Mechanism of Action
Clinical Uses
Adverse Effects
Posterior Pituitary Hormones
Oxytocin
Pharmacokinetics
Pharmacodynamics
Clinical Uses
Therapeutic Uses
Toxicity
Contraindications
Vasopressin
Pharmacokinetics
Pharmacodynamics
Clinical Use
Untoward Effects
Contraindications
REVIEW QUESTIONS
CHAPTER 5.2:
Thyroid and Antithyroid Drugs
THYROID HORMONES
Pharmacokinetics
Mechanism of Hormone Action
Physiologic Effects of Thyroid Hormones
Thyroid Preparations
Synthetic Preparations (Levothyroxine, Liothyronine and Liotrix)
Indications for Use of Thyroid Hormone
Hypothyroidism or Myxedema
Cretinism
Myxedema Coma
Benign Solitary Nodule
Simple Goiter and Hashimoto Thyroiditis
Drug-induced Hypothyroidism
Other Non-specific Uses
Diagnostic Uses
ANTITHYROID DRUGS
Thioamides
Mechanism of Action
Indications
Untoward Effects
Propylthiouracil
Methimazole
Anion Inhibitors
Iodides
Clinical Considerations
Major Disadvantages
Iodinated Radiographic Contrast Media
Clinical Use
Toxicity
Radioactive Iodine
Mechanism of Action
Therapeutic Advantages
Contraindication
Adrenergic Receptor Blocking Drugs
THYROID HORMONE DEFICIENCY
Hypothyroidism
Causes of Hypothyroidism
Classification of Hypothyroidism
Pathogenesis
Clinical Presentation
Laboratory Tests
Pharmacological Treatment
Thyrotoxicosis
Clinical Presentations of Thyrotoxicosis
Graves’ Disease
Clinical Presentations of Graves’ Disease
Diagnosis
Thyroid Storm
Treatment
REVIEW QUESTIONS
CHAPTER 5.3:
Adrenocorti-costeroids and their Antagonists
ADRENAL GLAND
ADRENOCORTICOSTEROIDS
General Features
Biosynthesis
Glucocorticoids
Mechanism of Action
Pharmacokinetics
Physiological Effects of Glucocorticoids (Cortisol)
Mineralocorticoids
Mechanism of Action
Uses of Mineralocorticoids
Overproduction of Mineralocorticoids
Physiological Effects of Mineralocorticoids
Synthetic Adrenocorticosteroids
Mechanism of Action
Pharmacodynamics
INDICATIONS FOR CORTICOSTEROIDS
Disorders of Adrenal Function
Acute Adrenal Insufficiency (Addisonian Crisis)
Primary Adrenal Insufficiency (Addison's Disease)
Secondary or Tertiary Adrenocortical Insufficiency
Congenital Adrenal Hyperplasia (Hyperfunction)
Cushing's syndrome
Non-adrenal Conditions
Acceleration of Lung Maturation
Diagnostic Purposes
Contraindications for Corticosteroid Use
Relative Contraindications
Adverse Effects of Corticosteroids
Toxicities Resulting from the Continued Use of the Corticosteroids
Sudden Withdrawal
Precautions Required During Chronic Administration of Corticosteroids
Salient Points Related to Corticosteroid Therapy
Diet and Corticosteroids therapy
ANTAGONISTS OF ADRENOCORTICAL AGENTS
Synthesis Inhibitors and Glucocorticoid Antagonists
Metyrapone
Aminoglutethimide
Trilostane
Formestane
Ketoconazole
Mifepristone
Eplerenone
Spironolactone
Mineralocorticoid Antagonist
Pharmacological Actions
Uses
Untoward Effects of Spironolactone
REVIEW QUESTIONS
CHAPTER 5.4:
Insulin
INSULIN
Proposed Mechanism of Insulin Secretion
Proposed Mechanism of Insulin Action
Receptor Activation
Action of Insulin at Target Sites
GLUCAGON
Clinical Uses
Untoward Effects
Diabetes Mellitus
Type 1 Diabetes
Type 2 Diabetes
INSULIN THERAPY
Insulin Preparations
Ultra-short or Rapid-acting Insulin Analogs
Short-acting Insulin
Intermediate-acting Insulin
Long-acting Insulin
Insulin Species
Human Proinsulin
Insulin Regimen
Delivery Systems
Indications for Insulin
Glycemic Control in Diabetes Mellitus
Daily Requirement of Insulin in Diabetes Mellitus Patients
Treatment of Diabetic Ketoacidosis or Diabetic Coma
Treatment of Non-ketotic Hyperglycemic Coma
Treatment of Diabetic Patients During Perioperative Period and Childbirth
Complications of Insulin Treatment
Treatment of Hypoglycemia
Immunopathology of Insulin Therapy
Drug Interactions
ORAL HYPOGLYCEMICS AGENTS
Sulfonylureas
Mechanism of Action
Pharmacokinetics
Drug Interactions
Untoward Effects
Advantages
Secondary Failure and Tachyphylaxis to Sulfonylureas
Meglitinides
Precautions
Repaglinide
Mechanism of Action
Pharmacokinetics
Drug Interactions
Untoward Effects
Precaution
Nateglinide
Advantages
Biguanides
Indications
Mechanism of Action of Biguanides
Pharmacokinetics
Dose
Advantages
Precautions
Untoward Effects
Contraindications
Thiazolidinedione Derivatives
Mechanism of Action
Clinical Effectiveness
Rosiglitazone (Avandia)
Pharmacokinetics
Untoward Effects
Precautions
Pioglitazone (Actos)
Adverse Effects
Alpha-glucosidase Inhibitors
Mechanism of Action
Clinical Uses
Untoward Effects
Dose
Treatment of Type 2 Diabetes Mellitus
REVIEW QUESTIONS
CHAPTER 5.5:
Gonadal Hormones and their Inhibitors
GONADAL HORMONES
OVARY
Puberty—Mechanism and Ovarian Function
Ovarian Cycle
Menopause
Anomalies in Ovarian Function
ESTROGENS
Estrogen Biosynthesis/Metabolism
Sites of Estrogen Synthesis
Physiological Effects of Estrogens
Metabolic Effects of Estrogen
Pharmacokinetics of Estrogens
Clinical Uses of Estrogen
Untoward Effects of Estrogen
Diethylstilbestrol
Contraindications
PROGESTINS
Synthetic Progestins
Mechanism of Action
Physiological Effects
Other Effects
Pharmacokinetics
Clinical Uses of Progestins
Therapeutic Uses (Fig. 5.5.7)
Other Uses
Diagnostic Uses
Untoward Effects of Progestins
OTHER OVARIAN HORMONES
Testosterone
Inhibin and Activin
Functions
Mechanism of Action
Clinical Uses
Relaxin
Physiological Effects
HORMONAL CONTRACEPTION
Mechanism of Action
Pharmacological Effects
Clinical Uses
Oral Contraception
Other Uses
Untoward Effects of Hormonal Contraceptives
Mild Effects
Moderate Effects
Severe Effects
Contraindications
Drug Interactions
Progestin Monotherapy
Beneficial Effects of Oral Contraceptives
ESTROGEN/PROGESTERONE INHIBITORS AND ANTAGONISTS
Tamoxifen
Clinical Uses
Untoward Effects
Stages of Breast Cancer
Stage I: Breast Cancer
Stage II: Breast Cancer
Stage IIIB: Breast Cancer
Stage IV: Breast Cancer
Mifepristone (RU-486)
Clinical Uses
Danazol
Mechanism of Action
Clinical Uses
Untoward Effects
Contraindications
OTHER OVARIAN INHIBITORS
Anastrozole
Letrozole/Fadrozole
OVULATION-INDUCING DRUGS
Clomiphene (Clomifene)
Mode of Action
Indications of Clomiphene in Females
Indications of Clomiphene in Males
Untoward Effects
Other Use
TESTES
Androgen (Anabolic Steroids)
Mechanisms of Action
Pharmacological Effects
Metabolism of Androgens
Physiological Effects
Synthetic Androgens
Clinical Uses of Testosterone and Its Derivatives
Untoward Effects
Contraindications
Androgen Suppression
Antiandrogens
REVIEW QUESTIONS
CHAPTER 5.6:
Agents Affecting Bone Mineral Homeostasis
INTESTINAL ABSORPTION
Calcium
Phosphorus
CALCIUM METABOLISM
PHOSPHATE METABOLISM
FLUXES OF CALCIUM AND PHOSPHATE
HORMONAL CONTROL SYSTEMS
Parathyroid Hormone
Calcitriol
Calcitonin
Hypoparathyroidism
Hyperparathyroidism
Vitamin D
Vitamin D Formulations
Drug Interactions
Calcitonin
Physiological Functions
Receptor
Pharmacokinetics
Clinical Uses
OSTEOPOROSIS
Treatment
Antiresorptive Agents
Bone anabolic Agents
Other Agents
SECTION 6: DRUGS USED TO TREAT DISEASES OF BLOOD
CHAPTER 6.1:
Drugs used in Disorders of Coagulation
MECHANISM OF BLOOD COAGULATION
Sequence
Regulation Factors
REGULATION OF COAGULATION AND FIBRINOLYSIS
Fibrinolysis
Drug Acting on Fibrinolytic System
ANTICOAGULANT DRUGS
Heparin
Mechanism of Action
Heparin: Standardized by Bioassay (Units)
Untoward Effects
Contraindications
Warfarin and Coumarin
Pharmacokinetics
Uses
Mechanism of Action of Coumarin
Untoward Effects of Coumarin
Drug-Drug Interactions of Oral Anticoagulants
Reversal of Warfarin Anticoagulant Effects
PHARMACOLOGICAL MANAGEMENT OF THROMBOSIS
Venous Thrombosis
Most Common is Genetic Risk Factor
Antithrombotic Management
Prevention
Oral Anticoagulants
Venous Thrombosis (Established)
Arterial Thrombosis
DRUGS USED IN BLEEDING DISORDERS
Vitamin K
Clinical Issues
Plasma Fractions in Bleeding due to Factor Deficiencies
Factor VIII Preparations
Factor IX
Fibrinogen
Fibrinolytic Inhibitors
Aminocaproic Acid (Amicar)
Serine Protease Inhibitors
Aprotinin
REVIEW QUESTIONS
CHAPTER 6.2:
Drugs used in Diseases of Hematopoietic System
ANEMIA
Signs and Symptoms
Classification of Anemia
Microcytic Hypochromic Anemia
Macrocytic Anemia
Macrocytic Hyperchromic Anemia
Pernicious Anemia
Normocytic Normochromic Anemia
Dimorphic Anemia
Hemolytic Anemia (Heinz Body Anemia)
Aplastic Anemia
DRUGS AFFECTING HEMATOPOIETIC SYSTEM
Hematinics
Ferrous Sulfate
Iron Dextran
Deferoxamine (Desferal)
Deferasirox
Folic Acid (Folvite)
Vitamin B12 (Cyanocobalamin or Hydroxocobalamin)
Hematopoietic Growth Factors
Epoetin Alfa (Erythropoietin, Epo—Epogen, Procrit)
Colony-Stimulating Factors
Megakaryocyte Growth Factors
SECTION 7: DRUGS AFFECTING OTHER SYSTEMS
CHAPTER 7.1:
Pulmonary Pharmacology: Asthma
DEFINITION OF ASTHMA
DIAGNOSIS
LONG-TERM CONTROL
QUICK RELIEF OF SYMPTOMS OR EXACERBATIONS SYMPTOMS
DRUGS USED IN THE TREATMENT OF ASTHMA
Sympathomimetic Drugs (Acting on β-adrenergic Receptors)
Isoproterenol (Isuprel)
Salbutamol
Terbutaline
Salmeterol and Formoterol
Methylxanthines
Pharmacological Actions of Methylxanthines
Theophylline
Anticholinergic Drugs (Muscarinic Antagonists)
Ipratropium Bromide (Atrovent and Apovent)
Corticosteroids
Mechanism of Action
Clinical Use
Untoward Effects
Advantages of Inhaled Corticosteroids
Mast Cell Stabilizers
Mechanism of Action
Cromolyn (Intal)
Nedocromil (Tilade)
Ketotifen
Leukotriene Pathway Inhibitors
Zileuton
Zafirlukast (Accolate)
Montelukast (Singulair)
Treatment of Status Asthmaticus
MEDICINES THAT LOOSEN LUNG SECRETIONS
Expectorants
Guaifenesin (Glyceryl Guaiacolate)
Ammonium Chloride
Sodium Citrate
Mucolytics
Acetylcysteine
Bromhexine
Ambroxol
POSTNASAL DRIP
Nasal Decongestion
REVIEW QUESTIONS
CHAPTER 7.2:
Gastrointestinal Drugs
ACID-PEPTIC DISEASES
GASTRIC PHYSIOLOGY
Physiological Stimulants
Physiologic Inhibition
DRUGS USED IN ACID-PEPTIC DISEASE
Drugs that Decrease Intragastric Acidity
Antacids
H2-Receptor Antagonists (Blockers)
Proton Pump Inhibitors
Anticholinergic Drugs
Prostaglandins Analogs
Drugs that Promote Mucosal Defense
Mucosal Protective Agents
Ulcer Healing Agents
Anti-Helicobacter Pylori Drugs
ANTIDIARRHEAL DRUGS
Loperamide (Lopex and Imodium)
Mode of Action
Contraindications
Drug-Drug Interactions
Diphenoxylate
Colloidal Bismuth Compounds (Bismuth Subsalicylate, Bismuth Subnitrate)
LAXATIVES
Bulk-forming Agents
Stool Softeners/Surfactants
Lubricants/Emollient
Hydrating Agents (Osmotics)
Osmotic Laxatives
Saline Laxatives
Hyperosmotic Agents
Stimulant and Irritant
Laxative Abuse
GASTROKINETIC (PROKINETIC) AGENTS
Bethanechol (Duvoid, Myotonachol and Urecholine)
Clinical Uses
Contraindications
Metoclopramide (Reglan) and Domperidone
Mechanism of Action
Pharmacological Actions
Clinical Uses
Untoward Effects
ANTIEMETIC DRUGS
Commonly used Antiemetic Drugs
Droperidol
Domperidone
Dolasetron
Ondansetron (Zofran)
Dronabinol (Marinol)
Scopolamine and Dimenhydrinate
Emetics
REVIEW QUESTIONS
CHAPTER 7.3:
Anthelmintic Drugs
CHEMOTHERAPY OF HELMINTHIC INFECTIONS
DRUGS FOR THE TREATMENT OF NEMATODES
Mebendazole (Ovex, Vermox, Antiox, Pripsen)
Mechanism of Action
Drug Interactions
Contraindications
Thiabendazole
Mechanism of Action
Untoward Effects
Pyrantel Pamoate
Mechanism of Action
Levamisole
Piperazine
Dose
Untoward Effects
Contraindications
DRUGS FOR THE TREATMENT OF CESTODES
Albendazole (Albenza, Eskazole, Zentel)
Other Uses
Mechanism of Action
Dose
Untoward Effects
Drug Interactions
Contraindications
Niclosamide (Niclocide)
Mechanism of Action
Dose
Untoward Effects
DRUGS FOR THE TREATMENT OF TREMATODES
Oxamniquine
Pharmacokinetics
Mechanism of Action
Side Effects
DRUGS FOR THE TREATMENT OF TREMATODES AND CESTODES
Praziquantel
Dose
Untoward Effects
Contraindications
DRUGS FOR THE TREATMENT OF FILARIASIS
Treatment
Diethylcarbamazine
Mechanism of Action
Ivermectin
Mechanism of Action
Contraindications
Albendazole
SECTION 8: CHEMOTHERAPEUTIC DRUGS
CHAPTER 8.1:
Antibacterial Drugs
CLASSIFICATION
Bactericidal Drugs
Bacteriostatic Drugs
Inhibitors of Cell Wall Synthesis
Synthesis of Peptidoglycan
Inhibitors of Cell Membrane Synthesis
Inhibitors of Nucleic Acid Synthesis
Inhibitors of DNA Replication
Quinolones
Nitroimidazoles
Inhibitors of RNA Polymerase
Inhibitors of Nucleotide Metabolism
Inhibitors of Protein Synthesis
Inhibitors of 30S Subunit
Inhibitors of 50S Subunit
Inhibitors of Folate Metabolism
PROPOSED COMMON MECHANISM OF BACTERICIDAL ANTIBIOTICS
Inhibitors of Cell Wall Synthesis
β-lactam Antimicrobials
Penicillin G
Penicillins Resistant to Acid and β-lactamase
Clinical Use of β-lactam Antibiotics
CEPHALOSPORINS
Cephalosporins and their Spectrum of Pharmacological Action
First Generation Agents
Second Generation Agents
Third Generation Agents
Fourth Generation Agents
OTHER β-LACTAM CONTAINING ANTIBACTERIALS
Aztreonam (Azactam)
Contraindications
Imipenem
Meropenem
Contraindications
Clavulanic Acid, Sulbactam, Tazobactam
OTHER INHIBITORS OF CELL WALL SYNTHESIS
Vancomycin
Major Clinical Uses
Bacitracin
Major Clinical Use
Adverse Effects
Cycloserine
Major Clinical Use
Adverse Effects
Membrane-active Agents
Polymyxins
Gramicidin
Inhibitors of Protein Synthesis
Aminoglycosides
Chloramphenicol (Chloromycetin)
Macrolides (Erythromycin and Azithromycin)
Tetracycline (Aureomycin, Terramycin and Panmycin)
AMINOGLYCOSIDES
Pharmacokinetics
Development of Resistance to Aminoglycosides
Adverse Effects
Streptomycin
Clinical Uses
Adverse Reactions
Gentamicin (Garamycin)
Clinical Uses
Adverse Reactions
Tobramycin (Nebcin)
Adverse Reactions
Amikacin (Amikin)
Clinical Uses
Adverse Reactions
Kanamycin and Neomycin
Clinical Uses
Spectinomycin (Trobicin)
CHLORAMPHENICOL, TETRACYCLINES AND CLINDAMYCIN
Chloramphenicol (Chloromycetin)
Clinical Uses
Adverse Effects
Tetracyclines
Mechanism of Bacterial Resistance to Tetracyclines
Clinical Uses
Adverse Reactions
Clindamycin (Cleocin)
Clinical Uses
Mechanism of Bacterial Resistance to Clindamycin
Adverse Reactions
MACROLIDES
Clinical Use
Adverse Reactions
Mechanisms of Bacterial Resistance
DISRUPTERS OF NUCLEIC ACID SYNTHESIS
Fluoroquinolones
Clinical Uses
Commonly Used Drugs
Adverse Reactions and Interactions
Ciprofloxacin (Cipro) and Levofloxacin (Levaquin)
Pharmacokinetics
Clinical Uses
Adverse Reactions
Rifamycins
Clinical Uses
Adverse Effects
Pharmacokinetics
Drug Interactions
Metronidazole
Mechanism of Action
Clinical Uses
Contraindications
Untoward Effects
Pharmacokinetics
Drug Interactions
SULFA DRUGS
Inhibitors of Folate-dependent Pathways
Mechanism of Action
Sulfonamides
Pharmacokinetics
Clinical Uses
Adverse Reactions
Trimethoprim
Clinical Uses
Adverse Effects
BACTERIAL RESISTANCE TO ANTIBIOTICS
CATIONIC PEPTIDES
Mechanisms of Action
Action of Cationic Peptides on Outer Membrane
Action of Cationic Peptides on Cytoplasmic Membrane
Clinical Uses
Role in Immunity
REVIEW QUESTIONS
CHAPTER 8.2:
Antimycobacterial Agents
TUBERCULOSIS
Tuberculosis in Pregnancy
Tuberculosis in AIDS Patients
Chemoprophylaxis
Mantoux Test (Purified Protein Derivative)
ANTITUBERCULAR DRUGS
CLINICAL USES
CLASSIFICATION
First-line Drugs
Isoniazid
Rifampin (Rimactane)
Ethambutol (Myambutol)
Streptomycin
Pyrazinamide
Other Drugs
Dapsone
Clofazimine (Lamprene)
Clarithromycin (Biaxin)
Azithromycin (Zithromax)
Thalidomide
RATIONALE AND EVIDENCE FOR THE STANDARD REGIMEN
Monitoring, DOTS and DOTS-Plus
DRUG-RESISTANT TUBERCULOSIS
TUBERCULOSIS OF THE CENTRAL NERVOUS SYSTEM
USE OF STEROIDS IN TREATING TUBERCULOSIS
REVIEW QUESTIONS
CHAPTER 8.3:
Antiviral Drugs
ACTION OF ANTIVIRAL DRUGS ON LIFE CYCLE OF VIRUS
LIMITATIONS OF VACCINES
Treatment of Viral Infections
Antiviral Targeting
Targeting the Specific Life Cycle Stage of Virus
Blocking the Viral Binding to Host Cell Receptor
Uncoating Inhibitors
Synthesis of Viral Components
Reverse Transcription
Integrase
Transcription
Translation/Antisense
Translation/Ribozymes (Nucleases)
Protease Inhibitors
Assembly
Release Phase
Stimulation of Host Immune System
Drugs Used in the Treatment of AIDS
HIGHLY ACTIVE ANTIRETROVIRAL THERAPY
Nucleoside Reverse Transcriptase Inhibitors
Zidovudine (Azidothymidine, AZT Retrovir)
Lamivudine (3TC Epivir)
Stavudine (D4T Zerit®)
Abacavir (Ziagen)
Non-nucleoside Reverse Transcriptase Inhibitors
Nevirapine (Viramune)
Delavirdine (Rescriptor)
Efavirenz (Sustiva)
Protease Inhibitors
Indinavir (Crixivan)
Nelfinavir (Viracept)
Lopinavir/Ritonavir (Kaletra)
Amprenavir (Agenerase)
Integrase Inhibitor
Fusion Inhibitors
Enfuvirtide (T-20 Fuzeon)
Immune Modulators
Interleukin-2
TREATMENT OF PNEUMONIA IN AIDS
Trimetrexate (Neutrexin)
Mechanism of Action
Clinical Uses
Contraindications
Untoward Effects
Drug Interactions
REVIEW QUESTIONS
CHAPTER 8.4:
Antifungal Drugs
FUNGAL INFECTIONS
Classes of Antifungal Drugs
SYSTEMIC ANTIFUNGAL DRUGS FOR SYSTEMIC MYCOSES
Amphotericin B
Pharmacokinetics
Mechanism of Action
Antifungal Activity
Clinical Uses
Dose
Drug Interactions
Untoward Effects
Caspofungin
Mechanism of Action
Untoward Effect
5-Flucytosine
Untoward Effects
Ketoconazole
Mechanism of Action
Antifungal Activity
Clinical Use
Common Untoward Effects
Drug-drug Interactions
Fluconazole (Diflucan)
Clinical Use
Untoward Effects
Drug-drug Interactions
Itraconazole (Sporanox)
Clinical Use
Drug-drug Interactions
Untoward Effects
DRUGS FOR CUTANEOUS MYCOSES
Griseofulvin
Mechanism of Action
Clinical Use
Adverse Effects
Terbinafine
Untoward Effects
Drug-drug Interaction
Nystatin
Miconazole
Mechanism of Action
Untoward Effects
TOPICAL DRUGS
Imidazoles and Triazoles
Polyene Macrolide Antibiotics
FUNGAL INFECTIONS IN HIV
Candidiasis
Range of Infections in HIV Patients
Treatment
Cryptococcosis
Common Symptoms
Treatment
Histoplasmosis
Clinical Presentations
REVIEW QUESTIONS
CHAPTER 8.5:
Antiprotozoal Drugs
ANTIMALARIAL DRUGS
PARASITIC LIFE CYCLE
CLASSIFICATION OF ANTIMALARIAL DRUGS
CLASSIFICATION BASED ON SITE OF DRUG ACTION AND PARASITE LIFE CYCLE
MALARIA CHEMOPROPHYLAXIS
TREATMENT OF MALARIA
Tissue Schizonticides
Primaquine
Blood Schizonticides
Chloroquine
Mefloquine
Quinine and Quinidine
Quinidine Gluconate
Artemisinin
Blood Schizonticides and Sporontocide
Pyrimethamine and Proguanil
Sulfonamides and Sulfones
DRUGS AGAINST PNEUMOCYSTIS JIROVECII
Trimethoprim-sulfamethoxazole
Atovaquone
Pentamidine
DRUGS AGAINST TRICHOMONIASIS
Orally used Drugs
Intravaginally used Drugs
ANTIAMEBIC DRUGS
Life Cycle of E. histolytica
Drugs used to Treat Amebiasis
Systemic Tissue/Invasive Amebicides
Luminal Amebicides
Metronidazole
Tinidazole
Chloroquine
Emetine
Paromomycin
Diloxanide Furoate
DRUGS AGAINST LEISHMANIASIS
Life Cycle
Clinical Characteristics of Leishmaniasis
Pharmacological Management of Leishmaniasis
DRUGS AGAINST GIARDIASIS
Pharmacological Management of Giardiasis
CHEMOTHERAPY FOR TOXOPLASMOSIS
Treatment
Precaution
REVIEW QUESTIONS
CHAPTER 8.6:
Urinary Antiseptics
NITROFURANTOIN (FURADANTIN, MACROBID, MACRODANTIN, NITRO MACRO AND URANTOIN)
Pharmacology
Mechanism of Action
Clinical Uses
Dose
Adverse Effects
Precautions
NALIDIXIC ACID (NEVIGRAMON, NEGGRAM, WINTOMYLON)
Mechanism of Action
Dose
Adverse Effects
Drug Interactions
CHAPTER 8.7:
Cancer Chemotherapy
GOAL OF CANCER CHEMOTHERAPY
PROBLEMS WITH CANCER CHEMOTHERAPY
IMMUNOLOGICAL ASPECTS OF CANCER CHEMOTHERAPY
CATEGORIES OF CHEMOTHERAPY DRUGS
Stop the Synthesis of Building Blocks of DNA Molecule
Directly Damage the DNA in the Nucleus of the Cell
Effects the Synthesis or Breakdown of the Mitotic Spindles
ANTIMETABOLITES
Methotrexate
Clinical Uses
Untoward Effects
Resistance to Methotrexate
5-fluorouracil
Clinical Uses
Untoward Effects
Hydroxyurea
6-mercaptopurine
Untoward Effects
6-thioguanine
Untoward Effects
ALKYLATING AGENTS
First Mechanism
Second Mechanism
Third Mechanism
Cyclophosphamide
Untoward Effects
Busulfan (Myleran)
Untoward Effects
ANTIBIOTICS
Dactinomycin (Actinomycin D)
Clinical Uses
Untoward Effects
Doxorubicin
Bleomycin
Untoward Effects
MITOTIC DISRUPTORS
Taxanes (Paclitaxel and Docetaxel)
Paclitaxel
Untoward Effects
Platinums (Carboplatin and Cisplatin)
ENZYME ANTICANCER AGENT
L-asparaginase
Clinical Uses
Untoward Effects
HORMONES
Estrogens
Progestins
Androgens
Glucocorticoids
HORMONES ANTAGONISTS
Estrogen and Androgen Inhibitors (Tamoxifen and Flutamide)
Tamoxifen
Flutamide (Eulexin)
Gonadotropin-releasing Hormone Agonists (Leuprolide and Goserelin Zoladex)
Leuprolide and Goserelin
MONOCLONAL ANTIBODIES
Trastuzumab
Rituximab
Untoward Effects
Cetuximab
OTHERS
Retinoic Acid Derivatives
Clinical Uses
Adverse Effects
Imatinib
CELL CYCLE SPECIFIC CHEMOTHERAPEUTIC DRUGS
REVIEW QUESTIONS
CHAPTER 8.8:
Drugs Affecting the Immune System
T HELPER 1—CELL-MEDIATED IMMUNITY
INAPPROPRIATE IMMUNE RESPONSE
Hypersensitivity
Type I Hypersensitivity (Immediate Hypersensitivity)
Type II Hypersensitivity
Type III Hypersensitivity
Type IV or Delayed Type Hypersensitivity
Autoimmunity
Immunodeficiency Diseases
ANTIBODY REAGENTS
Vaccines and Antisera
Passive Immunization
Clinical Uses
Commonly Used Agents
Active Immunization
Clinical Uses
Commonly Used Agents
Untoward Effects of Vaccines and Antisera Administration
Antithymocyte Globulin
Mechanism of Action
Clinical Uses
Untoward Effects
Infliximab
Mechanism of Action
Clinical Uses
Untoward Effects
Dose
Daclizumab (Zenapax)
Mechanism of Action
Clinical Uses
Pharmacokinetics
Etanercept (Enbrel)
Mechanism of Action
Clinical Uses
Rho (D) Immunoglobulin
Clinical Use
Muromonab
Mechanism of Action
Antilymphocyte Globulin
IMMUNOSUPPRESSANTS
Azathioprine
Mechanism of Action
Short-term Untoward Effects
Long-term Untoward Effects
Cyclosporine
Clinical Uses
Adverse Effects and Interactions
Formulations
Tacrolimus
Mechanism of Action
Clinical Uses and Contraindication
Untoward Effects
Glucocorticoids
Anti-inflammatory
IMMUNOMODULATORS
Levamisole
Clinical Use
Administration and Metabolism
Bacillus Calmette-Guérin
Clinical Uses
Method of Administration
Other Uses
Adverse Effects
Aldesleukin (Proleukin)
Untoward Effects
SECTION 9: ANTI-INFLAMMATORY AND ANALGESIC DRUGS
CHAPTER 9.1:
Anti-inflammatory Drugs
NON-STEROIDAL ANTI-INFLAMMATORY DRUGS
Classification of NSAIDs Based on their Action
Aspirin
Mechanism of Action
Pharmacological Actions
Pharmacokinetics
Clinical Uses
Untoward Effects
Contraindications
Management of Toxicity Caused by Aspirin Overdosage
Drug-drug Interactions
Non-acetylated Salicylates
Diflunisal
Other Non-steroidal Anti-inflammatory Agents
Pharmacodynamics
Pharmacokinetics
Ibuprofen
Flurbiprofen
Ketoprofen
Oxaprozin
Naproxen and Fenoprofen
Diclofenac
Sulindac
Tolmetin
Etodolac
Nabumetone
Meclofenamate
Indomethacin
Clinical Uses
Untoward Effects
Contraindications
Acetaminophen (Paracetamol)
Pharmacokinetics
Clinical Uses
Untoward Effects
Phenylbutazone
Ketorolac
Nimesulide
Coxibs
REVIEW QUESTIONS
CHAPTER 9.2:
Antirheumatic Drugs
METHOTREXATE
Untoward Effects
CHLOROQUINE AND HYDROXYCHLOROQUINE
TUMOR NECROSIS FACTOR-ALPHA BLOCKING DRUGS
Etanercept
Adverse Effects
Infliximab
Adverse Effect
Adalimumab
GOLD COMPOUNDS
Pharmacokinetics
Pharmacodynamics
Clinical Uses
Untoward Effects
Contraindications
PENICILLAMINE
Pharmacokinetics
Pharmacodynamics
Clinical Uses
Drug Interaction
Untoward Effects
Adverse Effects
Contraindications
SULFASALAZINE
Pharmacokinetics
Pharmacodynamics
Uses
Untoward Effect
GLUCOCORTICOIDS
Pharmacodynamics
Untoward Effects
CHAPTER 9.3:
Drugs for Gout
GOUT
CLASSIFICATION OF DRUGS USED IN GOUT
Colchicine
Mechanism of Action
Clinical Uses
Untoward Effects
Non-steroidal Anti-inflammatory Drugs
Allopurinol
Pharmacodynamics
Clinical Uses
Untoward Effects
Drug-drug Interactions
Uricosuric Drugs
Pharmacodynamics
Drug Interactions
Untoward Effects
INDEX
TOC
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