Pharmacology study for Pharmaceutical Job Preparation
Drug Examples
* Acidic drugs (ABCD)
⇨ Aspirin
⇨ Barbiturates (Thiopental)
⇨ Cloxacilin
⇨ Diazepam
* Examples of Basic drugs (DIPA)
⇨ Digoxin
⇨ Isoprenaline
⇨ Penicillin
⇨ Atropine
* Example of Prodrugs
Prodrug ⇨ Active drug
Aspirin ⇨ Salicylic acid
Codeine ⇨ Morphine
Diazepam ⇨ Oxazepam
Levodopa ⇨ Dopamine
* Drug-drug Interactions
⇨ Antacid + Tetracycline ( Antacid reduce the absorption of tetracycline)
⇨ Digitalis + Thiaxide (Thiazide cause hypokalacemia and Digitalis toxicity increase)
⇨ Insulin + Propranolol (Hypoglycemic shock occurs)
⇨ Sulfonamide + Tolbutamide (Hypoglycemic shock occurs)
⇨ Warfarin + Vitamin K (Anti-coagulant effect of warfarin is prevented)
Examples of Anti Parkinson drugs
⇨ Bromocriptine
⇨ Carbidopa
⇨ Levodopa
* Examples of Anesthetic drugs:
⇨ Gallamine
⇨ Ketamine
⇨ Fentamine
⇨ Chlorprocaine
⇨ Succinylcholine
* Examples Anti-viral drugs:
⇨ Acyclovir
⇨ Ganciclovir
⇨ Famciclovir
* Examples Anti-fungal drugs:
⇨ Amphotericin B
⇨ Fluconazole
⇨ Itraconazole
* Examples Bronchodilators:
⇨ Albuterol
⇨ Isoproterenol
⇨ Levalbuterol
* Examples of Anti-coagulants:
⇨ Clopidogrel
⇨ Heparin
⇨ Warfarin
* Examples of Thrombolytic drugs:
⇨ Streptokinase
⇨ Urokinase
⇨ Anistreplase
* Examples of H1 Blocker antihistamine:
⇨ Chlorpheniramine
⇨ Diphenhydrazine
⇨ Promethazine
* Examples of H2 blocker antihistamine:
⇨ Cimetidine
⇨ Famotidine
⇨ Ranitidine
* Examples of Proton Pump inhibitors:
⇨ Esomeprazole
⇨ Lansoprazole
⇨ Omeprazole
⇨ Pantoprazole
⇨ Rabeprazole
* Examples of Neuromuscular Blocking agents:
⇨ Gallamine (Gallamine is a non-depolarizing muscle relaxant.)
⇨ Pancuronium (Pancuronium is a neuromuscular blocker used as an adjunct to general anesthesia to facilitate tracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation.)
* Examples of Antiarrhythmic drugs:
⇨ Atenolol (Beta Blocker Drug)
⇨ Metoprolol
⇨ Verapamil
* Examples of Antihypertensive drugs:
⇨ Atenolol
⇨ Metoprolol
⇨ Verapamil (Verapamil is in a class of medications called calcium-channel blockers. It works by relaxing the blood vessels so the heart does not have to pump as hard. It also increases the supply of blood and oxygen to the heart and slows electrical activity in the heart to control the heart rate.)
* Examples of Antianginal drugs:
⇨ Atenolol
⇨ Metoprolol
⇨ Verapamil
* Examples of Anti-diabetic drugs:
⇨ Metformin
⇨ Phenformin
⇨ Buformin
⇨ Glipizide
⇨ Tolbutamide
* Examples of First generation anti-diabetic drugs:
⇨ Tolbutamide
* Examples of Second generation anti-diabetic drugs:
⇨ Glipizide
* Examples of Antacids:
⇨ Aluminium hydroxide
⇨ Magnesium hydroxide
⇨ Calcium carbonate
⇨ Sodium bicarbonate
* Examples of Teratogenic drugs:
⇨ Aspirin
⇨ Indomethacin (A non-steroidal anti-inflammatory drug commonly used to reduce pain, fever, stiffness and swelling.)
⇨ Tetracycline
⇨ Thalidomide
⇨ Warfarin
General Pharmacology
Absorption of Drugs
M/A of absorption of drug from GI tract
⇨ Passive diffusion
⇨ Facilitated diffusion
⇨ Active transport
⇨ Endocytosis
⇨ Exocytosis
* Factors influencing drug absorption
⇨ Effect of pH on drug absorption
⇨ Blood flow to the absorption site
⇨ Total surface area available for absorption
⇨ Contact time at the absorption surface
⇨ Expression of P-glycoprotein
⇨ Effect of food
Anaphylactic Shock
It is a serious type of immediate allergic reaction which needs immediate medical treatment.
Types of Anaphylaxis
Type I reaction: Immediate reaction
Type II reaction: Auto-allergy
Type-III: Complex mediated
Type-IV: Delayed reaction
Clinical features of Anaphylaxis shock
⇨ Respiratory distress
⇨ Dilation of pupil
⇨ Loss of consciousness
⇨ Low Blood pressure
⇨ Tightness in the chest
⇨ Circulatory failure
⇨ Imperciptible pulse
⇨ Death
* Mechanism of Anaphylaxis
⇨ Drug intake
⇨ Formation of tissue sensitizing Ab-IgE
⇨ Fixed to mast cells or leukocytes
⇨ Subsequent administration of same drug effects with IgE
⇨ Activate mast cells
⇨ Release of histamine, SRS-A (slow-reacting substance of anaphylaxis), Bradykinin, Serotonin, Prostaglandin
⇨ Produce Anaphylactic shock
*** pH
pH is the negative logarithm of hydrogen ion concentration
pH of Blood ⇨ 7.35-7.45
pH of Tear ⇨ 7.4
pH of Bile ⇨ 6-8.5
pH of Saliva ⇨ 5.5-7.5
pH of Skin ⇨ 5.5
pH of Urine ⇨ 4.5-8.00
pH of Gastric juice ⇨ 1.5-3.5
pH of HCl ⇨ 1.2-1. 4
Bioequivalence
Two drug formulations are bioequivalence if they show comparable bio-availability and similar times to achieve peak blood concentration.
Therapeutic equivalence
Two drug formulations are therapeutically equivalent if they are pharmaceutically equivalent
(that is, they have the same dosage form, contain the same active ingredient and use the same route of administration)
with similar clinical and safety profiles.
Therapeutics
The branch of pharmacology that deals with the art and science of treatment of disease.
It is the application of pharmacological information together with the knowledge of disease, for the prevention and cure of disease.
Pharmacogenomics
Pharmacogenomics is the broader application of genomic technologies to new drug discovery and further characterization of older drugs.
Pharmacoepidemiology
Pharmacoepidemiology deals with the effects of drugs on a large population.
The effects may be good or harmful.
Volume of distribution
The apparent volume of distribution is defined as the fluid volume that is required to contain the entire drug in the body at the same concentration measured in the plasma.
Pharmacodynamics ***
Pharmacodynamics describes the actions of a drug on the body and the influence of drug concentrations on the magnitude of the response.
Intrinsic activity of a drug
The intrinsic activity of a drug determines its ability to fully or partially activate the receptors.
Agonist ***
The term agonist refers to a naturally occuring small molecule or a drug that binds to a site on a receptor protein and activates it.
Classification of Agonists
⇨ Full agonists
⇨ Partial agonists
⇨ Inverse agonists
Full agonist
If a drug binds to a receptor and produces a maximal biologic response that mimics the responses to the endogenous ligand, it is called full agonist. [Mimics ⇨ অনুকরণকারী]
Antagonist ***
Antagonists bind to a receptor with high affinity but possess zero intrinsic activity.
An antagonist has no effect in the absence of an agonist but can decrease the effect of agonist when present.
Classification of Antagonists
⇨ Competitive antagonist
⇨ Irreversible antagonists
⇨ Allosteric antagonists
⇨ Functional antagonists
Potency
Potency is a measure of the amount of drug necessary to produce an effect of a given magnitude.
Efficacy
Efficacy is the magnitude of response a drug causes when it interacts with a receptor.
A drug with greater efficacy is more therapeutically beneficial than is on that is more potency.
Therapeutic Index***
The therapeutic index is a quantitative measurement of the relative safety of a drug.
The therapeutic Index of a drug is the ratio of the dose that produces toxicity in half of the population to the dose the produces a clinically desired or effective response in the half of the population.
TI = TD50/ED50
Different types of Pharmacopoeia:
⇨ British Pharmacopoeia
⇨ European Pharmacopoeia
⇨ French Pharmacopoeia
⇨ German Pharmacopoeia
⇨ Japanese Pharmacopoeia
⇨ Portugese Pharmacopoeia
⇨ United states Pharmacopoeia
⇨ Indian Pharmacopea
Drug
A drug is any substance that acts on the living body to alter the physiological process and are used for prevention, diagnosis, control and treatment of disease.
Medicine
Medicine is the formulated form of drug having definite dose, dosage form, leveling and packaging.
Drug vs Medicine
A drug is any substance that acts on the living body to alter the physiological process and are used for prevention, diagnosis, control and treatment of disease.
Medicine is the formulated form of drug having definite dose, dosage form, leveling and packaging.
Drug is a single active ingredient
Medicine contains more than one ingredient.
Drug has no form and dose.
Medicine has a suitable form and dose.
Drug is used for prevention, diagnosis and treatment.
Medicine is used for therapeutic treatment
Prodrug
The drugs which do not produce any pharmacological effect until they are chemically altered within the body are called prodrug.
Example of Prodrugs
Prodrug ⇨ Active drug
Aspirin ⇨ Salicylic acid
Codein ⇨ Morphine
Diazepam ⇨ Oxazepam
Levodopa ⇨ Dopamine
Classification of prodrugs:
Type-1 prodrugs
⇨ Bioactivated inside the cells.
⇨ Example: Aciclovir, Captopril, Carbamazepine, Fluorouracil
Type-2 prodrugs
⇨ Bioactivated outside the cells.
Examples: Acetylsalicylate,Bacampicillin, Bambuterol, Chloramphenicol
Purpose of using prodrug:
⇨ To avoid toxicity
⇨ To increase bioavailability.
Placebo
Placebo are inactive substance having no pharmacological effect given to satisfy patient's demand for medicine (Mental satisfaction)
Purpose of using placebo
⇨ For mental satisfaction of patient
⇨ For the treatment of drug addict patient.
Rational use of medicines:
Patients recieve medications appropriate to their needs, in doses that meet their own individual requirements, for an adequate period of time and at the lowest cost to them and their community.
Receptors
A receptor is a protein macrogmolecules embedded within the cell membrane with which messenger combine reversibly and/or irreversible in order to produce biological effect.
Drug + receptor ⇨ Drug-receptor compkex
Classification of receptors
According to location:
Type-1 receptor (Situated on the external surface of the plasma membrane of the target cell.)
Type-2 receptor (Situated in the cytoplasm of target cell)
Type-3 receptor (Situated in the nucleus of the target cell)
According to function:
1. Active receptor
⇨ About 1-2% of the receptor are active receptor.
⇨ Example: Chollinergic receptor, Muscarinic receptor, Histamin receptor
2. Silent receptor
⇨ Agonists may become attached but incapable of producing a pharmacological response.
⇨ Example: Plasma protein
3. Spare receptor
⇨ About 98-99% of te receptors are spare receptors.
⇨ When active receptors are saturated, they become active.
⇨ Example: Nicotinic receptor
Major receptor families:
1. Transmembrane ligand-gated ion channel
⇨ Collinergic-nicotinic receptors
2. G-protein-coupled receptors
⇨ Alpha & Beta adrenoceptors
3. Enzyme-linked receptors
⇨ Insulin receptors
4. Intracellular receptors
⇨ Steroid receptors
Examples of Monosaccharides: Glucose, Fructose
Examples of Oligosaccharides: Sucrose, Lactose, Maltose
Examples of Polysaccharides: Starch, Cellulose
Examples of Polysaccharide comples: Gums, Mucilage
Examples of Acidic drugs (ABCD)
⇨ Aspirin
⇨ Barbiturates
⇨ Cloxacillin
⇨ Diazepam
Examples of Basic drugs (DIPA)
⇨ Digoxin
⇨ Isoprenalin
⇨ Penicillin
⇨ Atropine
Isoprenaline
A sympathomimetic beta-adrenergic agonist medication, structurally similar to epinephrine and mainly used in treating bradycardia.
Digoxin
A purified cardiac glycoside extracted from the foxglove plant, Digitalis lanata, widely used in the treatment of heart conditions such as atrial fibrillation.
Atropine
An alkaloid extracted from the plant deadly nightshade (Atropa belladonna) and other sources.
Though overdoses would be fatal it is used as a drug in medicine for its paralytic effects (e.g. in surgery to relax muscles, in dentistry to dry the mouth, in ophthalmology to dilate the pupils).
Routes of Drug Administration
External routes
⇨ Oral route
⇨ Sublingual routes
⇨ Rectal route
Parenteral routes
⇨ Intravascular
⇨ Intramuscular
⇨ Subcutaneous
Other routs
⇨ Inhalation
⇨ Intranasal
⇨ Topical
⇨, Transdermal
Reactions of Drug metabolism
The kidney cannot efficiently be liminate lipophilic drugs that readily cross cell membranes and are reabsorbed in the distal convoluted tubules.
Therefore lipid soluble drugs are first metabolized into more polar substances in the liver via two general sets of reactions, called phase I and Phase II
Phase I reactions
Phase I reactions convert lipophilic drugs into more polar molecules by introducing or unmasking a polar functional group( -OH, NH2)
Phase I reactions usually involve reduction, oxidation or hydrolysis
The phase I reactions most frequently involved in drug metabolism are catalyzed by the cyp450 enzyme.
Phase II reactions
The phase II reaction consists of conjugation reactions.
NSAID (Non-steroidal Anti-Inflammatory drug)
⇨ NSAIDs are a class of drugs that provide analgesic and antipyretic effects and in higher doses, anti-inflammatory effects.
Anti-inflammatory effect
An effect that prevents or counteracts inflammation.
Inflammation
A condition of any part of the body, consisting of congestion of the blood vessels, with obstruction of the blood current, and growth of morbid tissue.
It is manifested outwardly by redness and swelling, attended with heat and pain.
Medicinal uses of NSAIDs
⇨ Rheumatoid arthritis
⇨ Osteoarthritis
⇨ Dysmenorrhoea (Painful menstruation)
⇨ Pyrexia (Fever)
⇨ Metastatic bone pain
Rheumatoid arthritis
A chronic and progressive disease in which the immune system attacks the joints.
It is characterised by pain, inflammation and swelling of the joints, stiffness, weakness, loss of mobility and deformity.
Tissues throughout the body can be affected, including the skin, blood vessels, heart, lungs, and muscles.
Osteoarthritis
A form of arthritis, affecting mainly older people, caused by chronic degeneration of the cartilage and synovial membrane of the joints, leading to pain and stiffness.
Arthritis
Inflammation of a joint or joints causing pain and/or disability, swelling and stiffness, and due to various causes such as infection, trauma, degenerative changes or metabolic disorders.
Classification of NSAIDs with example
1. Selective COX-2 inhibitors
⇨ Celecoxib
⇨ Rofecoxib
⇨ Valdecoxib
2. Salicylates
⇨ Aspirin
3. Acetic acid derivatives
⇨ Diclofenace (Painkiller)
⇨ Indomethacin (having Teratogenic effect)
⇨ Ketorolac (Used as an analgesic and antipyretic action)
Celecoxib
A non-steroidal anti-inflammatory drug used in the treatment of osteoarthritis, rheumatoid arthritis, acute pain, painful menstruation and menstrual symptoms, and to reduce numbers of colon and rectum polyps in patients with familial adenomatous polyposis.
Analgesic
Any medicine, such as aspirin, that reduces pain without inducing unconsciousness.
Adrenergic drugs (Adrenergic blocking drug/ Sympathomimetic drug)
Classification of Adrenergic drugs
1. Alpha adrenergic blocking drugs (Block alpha adrenergic receptors)
⇨ Phentolamine (Used in the treatment of erectile dysfunction)
2. Beta adrenergic blocking drugs (Block beta adrenergic receptors)
⇨ Acebutolol HCl (used in the treatment of hypertension and arrhythmias)
⇨ Atenolol (Used in the treatment of cardiovascular disease)
⇨ Metoprolol (Used in treatment of several diseases of the cardiovascular system, especially hypertension.)
3. Both alpha & beta adrenergic blocking drugs (Non selective beta blocker)
⇨ Carvedilol
⇨ Labetalol (Used in the treatment of high blood pressure.)
3. Antiadrenergic drugs (Block adrenergic nerve fibres within CNS or PNS)
Clonidine HCl ( Used in the treatment of hypertension, anxiety disorder, cancer pain, Menopusal flushing, Panic disorder; acting by stimulating alpha-2 receptor in the brain
Metoprolol
A selective β1 receptor blocker used in treatment of several diseases of the cardiovascular system, especially hypertension.
Clonidine
A drug traditionally prescribed for hypertension, having the chemical formula C9H9Cl2N3, and acting by stimulating α2 receptors in the brain
Adrenergic Agonists
Direct acting adrenergic agonists
⇨ Albuterol (Used to prevent and control bronchial airway obstruction in asthma and COPD.)
⇨ Clonidine
⇨ Dopamine (A neurotransmitter associated with movement, attention, learning, and the brain’s pleasure and reward system.)
⇨ Epinephrine
⇨ Norepinephrine (A neurotransmitter found in the locus coeruleus which is synthesized from dopamine.)
⇨ Isoproterenol (An aromatic amine, used as a sympathomimetic bronchodilator)
⇨ Phenylephrine
⇨ Salmaterol
Epinephrine
A catecholamine hormone and neurotransmitter;
as a hormone, secreted by the adrenal gland in response to stress (when it stimulates the autonomic nervous system);
as a neurotransmitter, synthesized from norepinephrine.
Indirect acting adrenergic agonists
⇨ Amphetamine
⇨ Cocaine
⇨ Tyramine (Used as a sympathomimetic agent)
Both direct & indirect acting adrenergic agents
⇨ Ephedrine (Used as a sympathomimetic drug)
⇨ Pseuephedrine (A sympathomimetic alkaloid commonly used as a decongestant)
Sympathetic nervous system
The part of the autonomic nervous system that raises blood pressure and heart rate, constricts blood vessels, and dilates the pupils when under stress.
Autonomic nervous system
The part of the nervous system that regulates the involuntary activity of the heart, intestines and glands.
These activities include digestion, respiration, perspiration, metabolism, and the modulation of blood pressure.
Viscera
Collectively, the internal organs of the body, especially those contained within the abdominal and thoracic cavities, such as the liver, heart, or stomach.
Classification of adrenoceptors
1. Alpha adrenoceptors (Alpha-1 and Alpha-2)
2. Beta adrenoceptors ( Beta-1 and Beta-2)
Pharmacologic action of Alpha-1 adrenoceptor (Adrenergic receptor)
⇨ Vasoconstriction (Constriction or narrowing of a blood vessel.)
⇨ Increased peripheral resistance
⇨ Increased blood pressure
⇨ Mydriasis (Dilation of the pupil of the eye)
⇨ Increased closure of internal sphincter of the bladder.
Pharmacologic action of Alpha-2 adrenoceptor
⇨ Inhibition of nor-epinephrine release
⇨ Inhibition of acetylcholine release
⇨ Inhibition of insulin release
Pharmacologi action of Beta-1 adrenoceptor
⇨ Tachycardia (Abnormal rapid heart rate)
⇨ Increased myocardial infarction
⇨ Increased release of renin
Pharmacologi action of Beta-2 adrenoceptor
⇨ Vadodilation
⇨ Decreased peripheral resistance
⇨ Bronchodialation
⇨ Increased muscle and liver glycogenolysis
⇨ Increased release of glucagon
⇨ Relaxed uterine smooth muscle.
Adrenergic Antagonists
Alpha adrenergic blocking drugs
⇨ Block alpha adrenoceptors
⇨ Reduces sympathetic tone at the blood vessels
⇨ Decrease peripheral vascular resistance
Phenoxybenzamine ( Prevents vasoconstriction of peripheral blood vessels by endogenous catecholamines)
Phentolamine (Used in the treatment of erectile dysfunction)
Prazosin (Selective competitive alpha-1 receptor blockers/ Useful in the treatment of hypertension)
Terazosin (Selective competitive alpha-1 receptor blockers/ Useful in the treatment of hypertension)
Tamsulosin (Selective alpha-1 recptor blocker/ Useful in the treatment of benign prostatic hyperplasia)
Beta adrenergic blocking drugs
Non-selective beta adrenergic blocking agents
⇨ Propranolol (Used in the treatment of hypertension)
⇨ Nadolol (Used in the treatment of high blood pressure, migraine headaches, and chest pain.)
⇨ Timolol (used to treat high blood pressure and prevent heart attacks.)
Selective Beta-1 antagonists
⇨ Acebutolol HCl (used in the treatment of hypertension and arrhythmias)
⇨ Atenolol (Used in the treatment of cardiovascular disease)
⇨ Betaxolol (Used in the treatment of Glaucoma, Ocular hypertension)
⇨ Bisoprolol (Used in the treatment of Hypertension, Angina pectoris, Congestive heart failure)
⇨ Esmolol
⇨ Metoprolol ( A selective β1 receptor blocker used in treatment of several diseases of the cardiovascular system, especially hypertension.)
⇨ Nebivolol (Used in the treatment of heart failure, hypertension)
Both Alpha & Beta adrenergic blocking drugs
Carvedilol (Used in the treatment of angina pectoris, congestive heart failure, hypertension, Left ventricular dysfunction, myocardial infarction)
Labetalol (Used in the treatment of hypertension, hypotensive anaesthesia))
Antiadrenergic drugs (Prevent the effectsof adrenaline)
Clonidine HCl ( Used in the treatment of hypertension, anxiety disorder, cancer pain, Menopusal flushing, Panic disorder; acting by stimulating alpha-2 receptor in the brain
Central Nervous System
Sympathetic nervous system
The part of the autonomic nervous system that raises blood pressure and heart rate, constricts blood vessels, and dilates the pupils when under stress.
Classification of CNS acting drugs
1. CNS Stimulants (Neuroleptics)
2. CNS depressants (Sedatives, Hypnotics, Narcotics, General Anesthetics)
Classification of CNS stimulant drugs
1. Directly acting on CNS
2. Reflexly acting on CNS
⇨ Ammonia
⇨ Lobeline (Used as an aid to smoking cessation)
⇨ Nicotine (Used as an insecticides)
Classification of directing acting on CNS drugs
1. Cortical stimulants
2. Medullary Stimulants
3. Spinal Stimulants
1. Cortical stimulants
⇨ Aminophylline (Bronchodialetor)
⇨ Atropine
⇨ Caffeine
⇨ Cocaine
⇨ Ephedrine (Used as a sympathomymetic drug.)
⇨ Theophylline
2. Medullary Stimulants
⇨ Amiphenazole
⇨ Adrenaline
⇨ Bemegride
⇨ Leptazole
⇨ Picrotoxin
3. Spinal Stimulants
⇨ Brucine
⇨ Strychnine (Used a pesticide)
⇨ Thebaine
Classification of CNS depressants
1. Sedatives
⇨ Diazepam
⇨ Oxazepam (Used to treat anxiety, insomnia and alcohol withdrawal)
2. Hypnotics (Inducing sleep)
⇨ Clobazepam
⇨ Clorazepam
⇨ Nitazepam
3. Narcotics
⇨ Codeine ( used as a hypnotic, analgesic and cough suppressant)
⇨ Morphine
⇨ Thebaine
4. General anesthetics
⇨ Chloroform
⇨ Ethylene
⇨ Halothane
⇨ Nitrogen di-oxide
Anesthetic drugs
1)Local anesthetic drugs
⇨ Articaine HCl
⇨ Bupivacaine HCl
⇨ Prilocaine HCl
General Anesthetics
⇨ Ancuronium bromide
⇨ Atracurium besylate
⇨ Doxacurium chloride
⇨ Succinylcholine chloride
Sedatives & Hypnotics
Sedative
A sedative is a drug that produces relaxing, calming effect.
Sedatives are usually given during datime hours
Although sedatives make the patient drowsy, they usually do not produce sleep.
Hypnotics
A hypnotic is a drug that induces sleep
Hypnotics allows the patient to fall asleep and stay sleep
Hypnotics may also called soporifics.
Hypnotics are given at night or hour of sleep.
Classification of Sedatives & Hypnotics
1. Barbiturates and miscellaneous sedatives
2. Hypnotics (Benzodizepines)
Classification of Barbiturates (Act as sedatives)
1) Ultra Short acting barbiturates: Thiamylal, Thiopental
⇨ Thiamylal (Status epilepticus, Induction of anesthesia, Reduction of intracranial pressure)
⇨ Thiopental
2) Short acting barbiturates: Pentobarbital, Secobarbital
⇨ Pentobarbital
⇨ Secobarbital
3) Intermediate acting barbiturates: Amobarbital, Aprobarbital, Butabarbital
⇨ Amobarbital
⇨ Aprobarbital
⇨ Butabarbital
4) Long-acting barbiturates: Mephobarbital, Phenobarbital
⇨ Mephobarbital
⇨ Phenobarbital
Examples of Benzodiazepines (Act as hypnotics/ also called antianxiety drugs/ used in the treatment of anxiety, insomnia etc)
⇨ Clonazepam ( Panic disorder, Epilepsy & other seizure disorder including status epileptic, tardive dyskensia, restless leg syndrome, rapid eye movement, burning mouth syndrome)
⇨ Estazolam (Used in the treatment of insomnia)
⇨ Flurazepam (Used in the treatment of insomnia)
⇨ Quazepam
Antidepressants
Depression
Depression is characterized by feeling of intense sadness, helplessness, worthlessness and impaired functioning.
Symptoms of depressions
⇨ Appetite disturbance
⇨ Sleep disturbance
⇨ Loss of interest in job, family and other activities usually enjoyed
Classification of Antidepressants:
1) Tricyclic antidepressants
2) Monoamine oxidase inhibitors (MAOIs)
3) Selective serotonine reuptake inhibitors (SSRIs)
4) Serotonin Reuptake inhibitors
5) Atypical Antidepressants
1) Tricyclic antidepressants
⇨ Amitriptyline
⇨ Amoxapine
⇨ Doxepine
⇨ Clomipramine
⇨ Desipramine
⇨ Doxepine
⇨ Imipramine
⇨ Trimipramine
⇨ Maprotiline
⇨ Amitriptyline
⇨ Nortriptyline
⇨ Protriptyline
2) Monoamine oxidase inhibitors (MAOIs)
⇨ Isocarboxazid
⇨ Phenelzine
⇨ Selegiline
⇨ Tranylcypromine
3) Selective serotonine reuptake inhibitors (SSRIs)
⇨ Citalopram
⇨ Escitalopram
⇨ Fluoxetine
⇨ Fluvoxamine
⇨ Paroxetine
⇨ Sertraline
4) Serotonin Reuptake inhibitors
⇨ Desvenlafaxine
⇨ Duloxetine
⇨ Levomilnacipran
⇨ Venlafaxine
5) Atypical Antidepressants
⇨ Bupropion
⇨ Mirtazapine
⇨ Nefazodone
Anesthetic drugs
Anesthesia
Anesthesia is a loss of feeling or sensation.
Classification of Anesthetic drugs
1. Local anesthetic
2. General Anesthetics
1)Local anesthetic drugs
⇨ Articaine HCl
⇨ Bupivacaine HCl
⇨ Chloroprocaine
⇨ Prilocaine HCl
General Anesthetics
⇨ Ancuronium bromide
⇨ Atracurium besylate
⇨ Doxacurium chloride
⇨ Succinylcholine chloride
⇨ Chloroform
⇨ Ethylene
⇨ Halothane
⇨ Nitrogen di oxide
Neuromuscular Blocking Agents
⇨ These drugs block cholinergic transmission between motor nerve ending and the nicotinic receptors on the skeletal muscle.
⇨ Neuromuscular blocking agents bind to acetylcholine receptors postsynaptically and inhibit the action of acetylcholine.
⇨ This blocks causes paralysis of the muscle.
⇨ Neuromuscular blocking agents are used as an adjacent to anesthesia in order to prevent movement of muscle during surgery.
⇨ These drugs provide complete muscle relaxation at lower doses, allowing for more rapid recovery from anaesthesia and reducing postoperative respiratory depression.
Classification of Neuromuscular blocking agents
1. Nondepolarizing blockers
2. Depolarizing agents
Nondepolarizing blockers:
⇨ Cisatracurium
⇨ Pancurium
⇨ Rocuronium
⇨ Vecuronium
Depolarizing agents
⇨ Succinylcholine
Histamines and Antihistamines
Histamine
⇨ Histamine is a potent biogenic amine.
⇨ Plays an important role in inflammation, anaphylaxis, allergies, gastric acid secretion and drug reaction.
⇨ Formed by decarboxylation of histidine
⇨ Released during allergic reactions
⇨ Causes:
i) Dilatation of capillaries
ii) Contraction of smooth muscles
iii) Stimulation of gastric acid secretion
Sources of histamines
⇨ Mast cell
⇨ Basophil
⇨ Leucocytes
⇨ Platelet
⇨ Gastric parietal cell
⇨ Neurons of CNS
⇨ Peripheral nerve fibres
Blood
Site of histamine releasing cells
⇨ GIT
⇨ Skin
⇨ Liver
⇨ Lungs
⇨ Uterine tubules
⇨ Brain
⇨ Arterioles
⇨ Capillaries
Antihistamines (Counteract the effect of histamine)
A) H1 receptor blockers
a) Potent & marked sedative (Promethazine, Dipheniramine)
b) Potent and moderate sedative ( Chlorpheniramine, Chlorcyclizine)
c) Less potent and less sedative (Mepyramine, Pheniramine Maleate)
B) H2 receptor blockers
A) H1 receptor blockers
⇨ Dipheniramine HCl
⇨ Dimen hydrinate
⇨ Promethazine HCl
⇨ Chlorpheniramine
⇨ Chlorcyclizine
⇨ Tetrahydroxy Carboline
⇨ Pheniramine Maleate
⇨ Mepyramine
2) Anti-emetic & anti-motion sickness
⇨ Dimenhydrinate
⇨ Diphenhydramine
⇨ Hydroxyzine
⇨ Promethazine
3) Anti-Parkinsonism
⇨ Orphenadrine
⇨ Phenindamine
B) H2 receptor blockers
⇨ Buriamide
⇨ Cimetidine (inhibits the production of acid in the stomach, mainly used to treat heartburn and peptic ulcers, but notorious for causing male impotence.
⇨ Famotidine
⇨ Lafutidine
⇨ Nizatidine
⇨ Ranitidine (Prevent the secretion of gastric acid)
H1 receptor blockers vs H2 receptor blockers
H1: Imidazole ring structure is extensively modified by other substituent.
H2: Imidazole part is reserved and the side chain is extensively modified.
H1: Compete for H1 receptor
H2: Compete for H2 receptor
H1: More lipid soluble, so crosses BBB & causes sedation.
H2: Less lipid soluble, so no sedation
H1: No effect on gastric secretion
H2: Inhibit gastric secretion
H1: Has many diverse use.
H2: Mainly use in peptic ulcer
H1: Example- Promethazine HCl, Chlorheniramine
H2: Example- Cimetidine, Ranitidine
Asthma
Asthma is a reversible obstructive disease of the lower airway.
Casuse of asthma:
⇨ Bronchospasm
⇨ Bronchoconstriction
⇨ Inflammation of the lining of bronchioles
⇨ Edema of the lining of the bronchioles
⇨ Production of thick mucus that can plug the airway
Types of Astma
1. Extrinsic asthma
2. Intrinsic asthma
3. Mixed asthma
Bronchodilators (Used to dilate and relax the bronchial passages and ease the flow of air to the lungs)
Bronchodialator
Bronchodialator is a drug used to relieve bronchospasm associated with respiratory disorders such as bronchial asthma, chronic bronchitis and emphysema
Classification of Bronchodialators
1) Sympathomimetics
2) Xanthine derivatives
1) Sympathomimetics
⇨ Albuterol
⇨ Isoproterenol
⇨ Levalbuterol (Short acting bronchodilator)
2) Xanthine derivatives
⇨ Aminophylline
⇨ Theophylline ( (A methylxanthine drug used in therapy for respiratory diseases such as COPD and asthma.)
Anticoagulant (Prevent coagulation of blood)
Overal mechanism of action:
⇨ i) Inhibit the action of coagulation factors (heparin)
⇨ ii) Interfere with the synthesis of the coagulation factors (Vitamin K antagonists such as warfarin)
Anticoagulant drugs:
⇨ Argatroban
⇨ Apixaban
⇨ Bivalirudin
⇨ Clopidogrel
⇨ Dabigatran etexilate
⇨ Desirudin
⇨ Fondaparinux
⇨ Heparin
⇨ Prasugrel
⇨ Rivaroxaban
⇨ Warfarin
Thrombolytic drugs (Dissolve blood clot)
Overal mechanism of action:
⇨ All thrombolytic drugs act either directly or indirectly to convert plasminogen to plasmin, which in turn, cleaves fibrin, thus lysing thrombi.)
Thrombolytic drugs
1) Tissue plasminogen activators
⇨ Alteplase
⇨ Reteplase
⇨ Tenecteplase
2) Anistreplase
3) Streptokinase (Form streptokinase-plasminogen complex ⇨ Convert uncomplexed plasminogen to active plasmin)
4) Urokinase (Directly cleaves the arginine-valine bond of plasminogen to yield active plasmin.)
Alteplase
⇨ Serine protease
⇨ Has low affinity for free plasminogen in the plasma but Rapidly activates plasminogen that is bound to fibrin in the thrombus.
⇨ Alteplase is said to be " fibrin selective at low doses.
⇨ Alteplase is approved for the treatment of MI, Massive PE and acute ischemic stroke.
Streptokinase
M/A:
Streptokinase + Plasminogen
Streptokinase-Plasminogen complex
The complex Activate plasminogen to plasmin
⇨ Plasmin active fibrin
⇨ As a result fibrin degradation products occurs
Drugs used to treat bleeding
⇨ Aminocaproic acid
⇨ Tranexamic acid
⇨ Protamine sulfate
⇨ Vitamin K
Tranexamic acid
Tranexamic acid is 10 times more potent than aminocaproic acid.
Protamine sulfate
Protamine sulfate antagonizes the anticoagulant effects of heparin
The positively charged protamine interacts with negatively charged heparin⇨ forming a stable complex without anticoagulant activity.
Blood Diseases
Anaemia & Haematinics
Haematinics
Haematinics are agents which are used in the treatment of anaemia to increase RBC number
Classification Haematinics
1. Drugs used in treatment of iron deficiency anaemia
2. Drugs used in the treatment of megaloblastic anaemia
Drugs for iron deficiency anaemia
⇨ Ferrous gluconate
⇨ Ferrous fumarate
⇨ Ferrous sulphate
⇨ Ferrous succinate
⇨ Iron sorbitol
⇨ Riboflavin
Drugs for Megaloblastic Anaemia
⇨ Vitamin C
⇨ Folic Acid
⇨ Vitamin B12
Blood-borne pathogens
⇨ AIDS
⇨ Brucellosis
⇨ Hepatisis B
⇨ Malaria
⇨ Syphilis
⇨ Tuberculosis
Cardiovascular diseases
⇨ Stroke (occurs when the blood supply to a part of the brain is interrupted)
i) Ischemic stroke
ii) Hemorrhagic stroke
⇨ Heart attact (Occurs when the supply of blood and oxygen to an area of heart muscle is blocked, usually by a clot in a coronary artery)
⇨ Angina Pectoris
⇨ Congestive Heart failure (Impairs the ability of the heart to fill with or pump a suffient amount of blood throughout the body.)
⇨ Aneurysm (Dilation of blood vessel by more than 50% of the diameter of the vessel and can lead to instant death at anytime)
⇨ Hypertension
Antiarrhythmics
Class-1 antiarrhythmics (Na+ channel blockers)
⇨ Disopyramide
⇨ Flecainide
⇨ Lidocaine
⇨ Mexiletine
⇨ Procainamide
⇨ Propafenone
⇨ Quinidine
Class-11 antiarrhythmics (Beta adrenoreceptor blockers)
⇨ Atenolol
⇨ Esmolol
⇨ Metoprolol
Class-III Antiarrhythmics (K+ Channel blockers)
⇨ Amiodarone
⇨ Dofetilide
⇨ Dronedarone
⇨ Ibutilide
⇨ Sotalol
Class-IV antiarrhythmics (Ca2+ channel blockers)
⇨ Diltiazem
⇨ Verapamil
Other antiarrhythmic drugs
⇨ Adenosine
⇨ Digoxin
⇨ Magnesium sulfate
Antianginal Drugs
Classification of Antianginal drugs
A. Beta-blockers
⇨ Atenolol
⇨ Bisoprolol
⇨ Metoprolol
⇨ Propanolol
B. Dihydropyridine Calcium Channel Blockers
⇨ Amlodipine
⇨ Felodipine
⇨ Nifedipine
C. Nondihydropyridine Calcium Channel Blockers (Can worsen heart failure due to their negative inotropic effect.)
⇨ Diltiazem
⇨ Verapamil
Verapamil
⇨ Slows atrioventricular conduction directly
⇨ Decrease heart rate, contractility, blood pressure and oxygen demand.
⇨ Has greater negative inotropic effect than amlodipine.
⇨ It is weaker vasodilator
⇨ Contraindicated in patient with pre-existing depressed cardiac function or atrioventricular conduction abnormalities.
D. Nitrates
⇨ Nitroglycerin
⇨ Isosorbide dinitrate
⇨ Isosorbide mononitrate
E. Sodium Channel Blockers
⇨ Ranolazine
Diabetes
Types of diabetes
1. Type 1 diabetes (Insulin dependent diabetes/Diabetes mellitus)
2. Type 2 Diabetes (The body does not produce enough insulin)
3. Gestational Diabetes (During pregnancy)
Antidiabetic drugs
Classification of antidiabetic drugs
1. Sufonylureas (Stimulate insulin secretion)
⇨ Glimepirile
⇨ Glipizide
⇨ Glyburide
2. Biguanides (Decrease hepatic production of glucose)
⇨ Metformin
3. Glinides (Stimulates insulin secretion)
⇨ Nateglinide
⇨ Repaglinide
4. Thiazolidinediones ( Decrease insulin resistance by binding to peroxisome proliferator-activated receptor-gamma in muscle, fat and liver.)
⇨ Pioglitazone
⇨ Rosiglitazone
5. Alpha-Glucosidase inhibitors (Decrease glucose absorption)
⇨ Acarbose
⇨ Miglitol
6. Dipeptidyl peptidase-4 (DPP-4) inhibitors ( Increase glucose-dependent insulin release and decreases secretion of glucagon)
⇨ Alogliptin
⇨ Linagliptin
⇨ Sitagliptin
⇨ Saxagliptin
7. Incretin mimetics ( Increase glucose-dependent insulin release and decreases secretion of glucagon)
⇨ Exenatide
⇨ Liraglutide
8. Sodium-glucose cotransporter-2 inhibitors ( Increases urinary glucose excretion)
⇨ Canagliflozin
⇨ Dapaglifozin
Types of Insulin
⇨ Insulin aspart
⇨ Insulin determir
⇨ Insulin glargine
⇨ Insulin glulisine
⇨ Insulin lispro
⇨ NPH insulin suspension
⇨ Regular insulin
Mechanism of Insulin
Binding of insulin with alpha-subunit of insulin receptor
Auto phosphorylation of brta suunit of insulin receptor
Activation of beta subunit
Activation of some enzymes in the cell & perform all activities of insulin
Gastric acidity
Drugs for Gastric acidity
1) Antacids
Aluminium hydroxides
Magnesium hydroxides
Calcium carbonare
Sodium bicarbonate
2) Proton pump inhibitors
Esomeprazole
Lansoprazole
Omeprazole
Pantoprazole
Rabeprazole
3) H2 receptor antagonistics
⇨ Cimetidine
⇨ Famotidine
⇨ Nizatidine
⇨ Ranitidine
H2 blocker vs PPI
H2: Block H2 receptors of the gastric parietal cells and inhibit HCl secretion.
PPI: Inhibit proton pump by inhibiting H+, K+, ATPase channels
H2: Inhibit both basal and food stimulated acid secretion about 97%
PPI: Inhibit both basal and food stimulated acid secretion about 100%
H2: Ineffective in H2 antagonist resistance patients.
PPI: Effective in H2 antagonist resistance patients.
H2: Relatively short duration of action
PPI: Having long-lasting effect on acid secretion
H2: Acid environment is not required for activation.
PPI: Activated at acific pH
Antihyperlipidemic drugs
1. HMG CoA Reductase inhibitors
⇨ Atorvastatin
⇨ Fluvastatin
⇨ Lovastatin
⇨ Pitavastatin
⇨ Pravastatin
⇨ Rosuvastatin
⇨ Simvastatin
2. Niacins
3. Fibrates
⇨ Fenofibrate
⇨ Gemfibrozil
4. Cholesterol Absorption inhibitors
⇨ Ezetimibe
5. Bile acid Sequestants
⇨ Colesevelam
⇨ Colestipole
⇨ Cholestyramine
5. Omega-3 Fatty acids
⇨ Docosahexaenoic acid
⇨ Eicosapentaenoic acid
⇨ Icosapent ethyl
Niacin
⇨Niacin can reduce LDL-C by 10 to 20%.
⇨ Most effective agent for increasing HDL-C.
⇨ It also lowers triglycerides by 20 to 35% at typical doses of 1.5 to 3 gms/day.
Cholestyramine
⇨ Anion-exchange resin.that bind negatively charged bile.acids and bile salts in the small intestine.
⇨ The resin/bile acid complex is excreted in the feces, thus lowering the bile acid concentration.
Respiratory Diseases Treatment
Respiratory disease
⇨ Asthma
⇨ COPD (Chronic obstractive pulmonary disease)
⇨ Allergic rhinitis
⇨ Cough
Drugs for Cough
⇨ Benzonatate
⇨ Codeine
⇨ Dextromethorphan
⇨ Guaifenesin
Drugs for Alergic rhinitis
Antibiotic drug
Bacteriostatic drugs
Bacteriostatic drugs arrest the growth and replication of bacteria at serum or urine levels achievable in patient.Thus limiting the spread of infection until the immune system attacks, immbobilizes abd eliminates the pathogens. If the drug is removed before the immune system has scavenged the organisms, enough viable organisms may remain to begin a second cycle of infection.
Examples:
⇨ Chloramphenicol
⇨ Sulfonamide
⇨ Tetracycline
Bacteriocidal drugs
Bactericidal drugs kill bacteria at resum levels achievable in the patient.
Examples:
⇨ Cephalosporines
⇨ Penicillin
⇨ Rifampicin
Minimum inhibiltory concentration (MIC)
The minimum inhibitory concentration is the lowest antimicrobial concentration that prevents visible growth of an organism after 24 hours of incubation.
Minimum bactericidal Concentration (MBC)
The minimum bactericidal concentration is the lowest concentration of antimicrobial agent that results in a 99.9% decline in colony count after overnight broth dilution incubations.
The minimum bactericidal concentration is the lowest concentration of antimicrobial agent that kills 99.9% of bacteria.
Postantibiotic effect
The postantibiotic effect is a persistent suppression of microbial growth that occurs after levels of antibiotic have fallen below the minimum inhibitory concentration (MIC).
Antimicrobial agents exhibiting a long postantibiotic effect often require only one dose per day, particularly against gram negative bacteria.
Example of antimicrobial agents exhibiting long postantibiotic effect
⇨ Aminoglycosides (Streptomycin, Gentamycin)
⇨ Fluoroquinolones (Ciprofloxacin, Nalidixic acid)
Narrospectrum antibiotic agent
Chemotherapeutic agents acting only on a single or a limited group of microorganisms are called narrospectrum antibiotic.
Examples of narrospectrum antibiotic agent
⇨ Isoniazid– is active only against Mycobacterium tuberculosis.
Extended-spectrum antibiotics
Extended spectrum is the term applied to antibiotics that are modified to be effective against gram-positive organisms and also against a significant number of gram-negative bacteria.
Examples of Extended-sprectrum antibiotics
⇨ Ampicillin
Broad-specctrum antibiotics
Broad-spectrum antibiotic is an antibiotic that acts on the two major bacterial groups gram-positive and gram - negative or any antibiotic that acts against a wide range of disease-causing bacteria. These medications are used when a bacterial infection is suspected that the group of bacteria is unknown or when infection with multiple groups of bacteria is suspected.
Emperic therapy
Emperic therapy is a medical treatment based on experience. It is applied before the confirmation of a definite medical disgnosis.
Synergism effect
Certain combinations of antibiotics are more effective than either of the drugs used separately. this combined effect of drugs is termed as synergism effect.
Examples: Beta lactam antibiotics + aminoglycosides
Drug resistance
The ability of a microorganism that prevent or inhibit the action of antibiotic that are given for inhibiting or killing the growth of that microorganism is termed as drug resistance.
Multi-drug resistant bacteria
Multidrug resistant organisams are a type of antimicrobial resistant microorganism that are resistant to at least one antimicrobial drug in three or more antimicrobial categories.
Antimicrobial categories are classifications of antimicrobial agents based on their mode of action and specific to target organisms.
Examples:
Vancomycin resistant Enterococci
Methicillin resistant staphylococcus aureus
Extensively drug resistant bacteria
Extensively drug resistant bacteria are a type of multidrug resistant organisms that are resistant to at least one antimicrobial agent in all antimicrobial categories or two or fewer antimicrobial categories.
Pandrug resistant bacteria
Pandrug resistant bacteria are a type of multidrug resistant organisms that are resistant to all antimicrobial agent in all antimicrobial categories.
Examples:
⇨ Klebsiella pneumoniae
Beta lactamase ***
Beta lactamase is a type enzyme produced by microorganism that hydrolytically inactivate the beta-lactam ring of penicillins, cephalosporins and related drugs.
Acetyltransferase
Acetyltransferases are enzymes produced by bacterial microorganisms that inactivate an antibiotic by transfering an acetyl group to the antibiotic, such as chloramphenicol or aminoglycosides.
Esterase
Esterases are enzymes produced by bacterial microorganisms that inactivate the macrolides antibiotics by hydrolize the lactone ring of macrolides (Azithromycin, Clarithromycin, Erythromycin, Trlithromycin)
Superinfection ***
Drug therapy particularly with broad-spectrum antimicrobials or combinations of agents, can lead to alterations of the normal microbial flora of the upper respiratory, oral or intestinal and genitourinary tract permitting the overgrowth of opportunistic organisms specially fungi or resistant bacteria. this overgrowth of microorganisms is termed as superinfection.
Bacteriostatic antibiotics
⇨ Chloramphenicol
⇨ Sulfonamide
⇨ Tetracycline
Bacteriocidal antibiotics
⇨ Cephalosporines
⇨ Penicillin
⇨ Rifampicin
Broadspectrum Antibiotics (Affect wide variety of microbial species)
⇨ Carbapenems
⇨ Cephalosporins
⇨ Chloramphenicol
⇨ Fluoroquinolones
⇨ Tetracycline
Narrow spectrum antibiotics
⇨ Erythromycin
⇨ Penicillin G
Time-dependent killing antibiotics/Bactericidal
⇨ Clindamycin
⇨ Linezolid
⇨ Vancomycin
Concentration-dependent antibiotics
⇨ Daptomycin
⇨ Telavancin
Long post-antibiotic effect related drugs
⇨ Aminoglycosides (Gentamycin)
Short post-antibiotic effect related drugs
⇨ Clindamycin
⇨ Penicilin-G
⇨ Vancomycin
Antibiotics which are metabolized by liver
⇨ Erythromycin
Antibiotics which are mainly metabolized by kidney
⇨ Penicillin-G
⇨ Tobramycin
⇨ Vancomycin
Pregnancy risk Category-D related antibiotics (There is chance for potential harm to the fetus)
⇨ Tobramycin
Antibiotic Resistance
Antibiotic resistance occurs when an antibiotic has lost its ability to effectively control or kill bacterial growth.
There are three main ways by which resistance can occur:
1. By natural resistance in certain types of bacteria
2. By genetic mutation
3. By one species acquiring resistance from another.
Most gram-negative organisms are inherently resistant to vancomycin.
Drug resistance mechanism of Microorganisms against penicillins:
1. Beta-lactamase activity
2. Decreased permeability to the drugs
3. Altered PBPs
Mechanism of drug resistance
A. Genetic alterations leading to drug resistance
B. Altered expression of proteins in drug-resistant organisms
1. Modification of target sites (S. pneumoniae resistance to Beta-lactam antibiotics)
2. Decreased accumulation
3. Enzymatic inactivation
Beta-lactamase Enzyme
An enzyme produced by certain bacteria, responsible for their resistance to beta-lactam antibiotics such as penicillin.
Complications of Antibiotic therapy
⇨ Hypersensitivity
⇨ Direct Toxicity
⇨ Superinfections ( Broad-spectrum or combinations, can lead to alterations of the normal microbial flora of the upper respiratory, oral, intestinal and genitourinary tracts, permitting the overgrowth of opportunistic organisms.)
Classification of Antimicrobial drugs
A. Classified by the chemical structure
⇨ Beta lactam antibiotics (Contain beta-lacting ring/ Penicillins, Cephalosporins, Carbapenems, Monobactams)
⇨ Aminoglycosides
B. Classified by their mechanism of action
⇨ Cell wall synthesis inhibitors (Penicillins, Cephalosporins)
⇨ Protein synthesis inhibitors (Tetracyclines)
⇨ DNA gyrase inhibitors (Ciprofloxacin, Nalidixic acid)
⇨ Folate Synthesis inhibitors (Sulfonamides,
⇨ Folate reductase inhibitors
⇨ Urinary tract Antiseptics
⇨ Interfere with DNA synthesis (Acyclovir)
⇨ DNA function inhibitors (Metronidazole, Rifampin)
⇨ Causing leakage from cell membranes (Bacitracin, Polymyxins)
C. Classified by the activity against particular types of organisms
⇨ Antimycobacterial Drugs (Isoniazid)
⇨ Antifungal Drugs (Amphotericin B)
⇨ Antiprotozoal Drugs
⇨ Antehelmintic Drugs
⇨ Antiviral Drugs
D. Classified by the mode of action
⇨ Broad spectrum antibiotics (Cephalosporins)
⇨ Narrow spectrum antibiotics (Penicillin)
Cell wall synthesis inhibitors
⇨ Penicillins
⇨ Cephalosporins
⇨ Carbapenems
⇨ Monobactams
⇨ Beta-Lactamse Inhibitors
⇨ Vancomycin (Useful in the treatment of Methicillin resistant staphylococcus aureas (MRSA) and Methicillin-resistant staphylococcus epidermitis (MRSE))
⇨ Daptomycin
⇨ Televancin
⇨ Fosfomycin
⇨ Polymyxins
Penicillins
Mechanism of action of penicillins
⇨ Penicillin-binding proteins
⇨ Inhibition of transpeptidase
⇨ Production of Autolysins
Natural penicillin
Penicillin G (Benzyl Penicilin)
Penicillin V (Acid stable) (Phenoxymethyl Penicillin)
Penicillin VK
Antistaphylococcal Penicillins
⇨ Dicloxacillin
⇨ Methicillin
⇨ Nafcillin
⇨ Oxacillin
Beta lactamase resistant Penicillins
Cloxacillin
Dicloxacillin
Methicillin
Nafcillin
Oxacillin
Aminopenicillins
Amoxicillin
Ampicillin
Bacampicillin
Epicillin
Hetacillin
Metampicillin
Pivampicillin
Talampicillin
Carboxypenicillins
Carcenicillin
Ticarcillin
Narrow Spectrum Penicillins (Acting only on a single or a limited group of microorganisms)
⇨ Isoniazid (Active only against Mycobacterium tuberculosis)
⇨ Penicillin G
Extended Spectrum Penicillins (Efeective against both gram positive and gram negative microorganisms)
⇨ Ampicillin
⇨ Amoxicillin
⇨ Becampicillin
⇨ Carbenicillin
⇨ Mezlocillin
⇨ Piperacillin
⇨ Ticarcillin
Drug-drug interaction of penicillin
Penicillin + Aminoglycoside⇨ Penicillin deactivate aminoglycosides
Penicillin + Bacteriostatic drugs⇨ Bacteriostatic drug show antagonist effect against penicillin
Penicillin + Warfarin ⇨ Penicillin potentiate coagulant effect of warfarin
Cephalosporins
⇨ The cephalosporins are beta lactam antibiotics that inhibits the cell wall of bacteria
⇨ Cephalosporins tend to be more resistant than the penicillins to certain beta-lactames
⇨ Commercially available cephalosporins are ineffective against MRSA, L. monocytogenes, C. difficile and the enterococci.
Classification Cephalosporins
First generation (Active against gram positive bacteria/ Resistant to staphylococcal penicillinase/ Active against Proteus mirabilis, E.coli and K. pneumoniae)
Cefadroxil
Cefazolin
Cephalothin
Cephelexin
Cephradine
Second generation (Active against gram negative bacteria such ads H. influenzae, Enterobacter aerogenes, Neisseria/ Activity against gram-negative is less)
Cefaclor
Cefmetazole
Cefonicid
Cefotetan
Cefoxitin
Cefprozil
Cefuroxime
Third generation (Active against gram negative bacteria)
Cefiazidime
Cefixime
Cefoperazone
Cefotaxime ( Used in the treatment of meningitis)
Ceftazidine (Active against Pseudomonous aeroginosa)
Ceftriaxone (Used in the treatment of meningitis)
Moxalactam
[Caution: 3rd generation cephalosporins may cause collateral damage, meaning the induction and spread of antimicrobial resistance, Fluoroquinolone is also associated with collateral damage]
Fourth generation (Active against gram positive & gram negative bacteria)
Cefclidine
Cefepime (Effective against Streptococci, staphylococci, Enterobacter species, E.coli, K.pneumoniae, P.mirabilis, P.aeroginosa)
Cefluprenam
Cefpirome
Cefoselis
Flomoxef
Fifth generation/ Advanced generation
Ceftaroline fosamil (Prodrug of Ceftaroline)
Ceftobiprole
Ceftolozane
Drug-Drug interaction of cephalosporins
Cephalosporin + Aminoglycoside⇨ Increase nephrotoxicity (Toxicity that damage kidney)
Cephalosporin + Probenecid⇨ Inhibit tubular secretion
Cephalosporin + Alcohol⇨ Disulfiram effect
Carbapenems (Synthetic beta-lactam antibiotics)
⇨ Doripenem
⇨ Ertapenem
⇨ Imipenem (It is compounded with cilastatin to protect from metabolism by renal dehydropeptidase)
⇨ Meropenem
Monobactams
⇨ Aztreonam (Effective against Enterobacteriaceae and P.aeruginosa)
Beta Lactamase Inhibitors ( Inactivate beta-lactamase enzye of microorganism, thereby protecting the antibiotics/ Do not have significant antibacterial activity)
⇨ Clavulanic Acid
⇨ Sulbactam
⇨ Tazobactam
Polymixins
⇨ Polymixin A
⇨ Polymixin B/ Colistin
Protein Synthesis Inhibitors
Classification of Protein Synthesis inhibitors
A. Tetracyclines
B. Glyclycyclines
C. Aminoglycosides
D. Macrolides
E. Ketolides
F. Fidaxomicin
G. Chloramphenicol
H. Clindamycin
I. Quinupristin/ Dalfopristin
J. Linezolid
A. Tetracyclines
Bind reversively to the 30S subunit of the bacterial ribosome
Prevents binding of tRNA to the mRNA-ribosome complex
Inhibit bacterial protein synthesis/
Commonly used in the treatment of Acne and Chlamydia infections
⇨ Demeclocycline
⇨ Doxycycline
⇨ Minocycline
⇨ Tetracycline
B. Glyclycyclines
⇨ Tigecycline ( Exhibits bacteriostatic action by reversibly binding to the 30S ribosomal subunit and inhibiting protein synthesis)
C. Aminoglycosides
⇨ Amikacin
⇨ Gentamycin
⇨ Neomycin
⇨ Streptomycin
⇨ Tobramycin
D. Macrolides (Having macrocyclic lactone structure/ Irreversible bind to the site on the 50S subunit of the bacterial ribosome⇨ inhibit translocation steps of protein synthesis)
⇨ Azithromycin
⇨ Clarithromycin
⇨ Erythromycin
Azithromycin
⇨ More active against respiratory infections due to H.influenzae and Moraxella catarrhalis.
⇨ Preferred therapy for urethritis caused by Chlamydia trachomatis
⇨ Extensive use has resulted in growing streptococcus pneumoniae resistance.
⇨ May Used for post delivery surgery
E. Ketolides (Active against many macrolide-resistant gram-positive bacteria)
⇨ Telithromycin
F. Fidaxomicin
G. Chloramphenicol
H. Clindamycin
I. Quinupristin/ Dalfopristin
J. Linezolid
DNA Gyrase inhibitors
Fluoroquinolones:
⇨ Ciprofloxacin
⇨ Levofloxacin
⇨ Moxifloxacin
⇨ Nalidixic acid
⇨ Norfloxacin
⇨ Ofloxacin
Ciprofloxacin
⇨ Effective in the treatment of many systemic infections caused by gram-negative bacilli.
⇨ It has best activity against Pseudomonas aeruginosa and is commonly used in cystic fibrosis patients for this indication.
⇨ Its bioavailability about 80%
⇨ Traveler's diarhea caused be E.coli as well as typhoid fever caused by salmonella typhi can be effectively treated with ciprofloxacin.
⇨ Also used as a second-line agent in the treatment of tuberculosis.
Folate synthesis inhibitors
⇨ Sulfonamides (Sulfamethoxazole)
⇨ Trimethoprim
Folate reductase inhibitors
⇨ Pyrimethamine
⇨ Trimethoprim
Combine inhibitors of Folate synthesis & folate reductase
⇨ Cotrimoxazole (Trimethoprim + Sulfamethoxazole)
Urinary tract Antiseptics
⇨ Methenamine
⇨ Nitrofurantoin
Antimycobacterial drugs
Drugs used to treat first line tuberculosis
⇨ Ethambutol
⇨ Isoniazid
⇨ Pyrazinamide
⇨ Rifabutin
⇨ Rifampin
⇨ Rifapentine
Antifungal drugs (Used to kill or inhibit the growth of fungus)
⇨ Amphotericin B
⇨ Flucytosine
⇨ Fluconazole
⇨ Itraconazole
⇨ Posaconazole
⇨ Voriconazole
⇨ Echinocandins
2) Drugs for Cutaneous Mycotic Infections
⇨ Terbinafine
⇨ Griseofulvin
⇨ Nystatin
⇨ Imidazole
⇨ Ciclopirox
Antiprotozoal Drugs
For Amebiasis
⇨ Choroquine
⇨ Metronidazole
⇨ Tinidazole
For Malaria
⇨ Chloroquine
⇨ Mefloquine
⇨ Primaquine
⇨ Pyrimethamine
⇨ Quinine
For Trypanosomiasis
⇨ Benznidaxole
⇨ Fflornithine
⇨ Melarsoprol
For Leishamaniasis
⇨ Miltefosine
⇨ Sofium Stibogluconate
For toxoplasmosis
⇨ Pyrimethamine
For Giardiasis
⇨ Metronidazole
⇨ Nitazoxanide
⇨ Tinidazole
Anthelminyic Drugs
For Nematodes
⇨ Diethylcarbamazine
⇨ Ivermectin
⇨ Mebendazole
⇨ Pyrantel pamoate
⇨ Thiabendazole
For Trematodes
⇨ Praziquantel
For Cestodes
⇨ Albendazole
⇨ Niclosamide
Anti-Viral Drugs (Used for prophylaxis and treatment of viral diseases)
1) Treatment of respiratory virus infections
⇨ Amantadine
⇨ Ribavirin
⇨ Rimentadine
2) Treatment of Herpes and cytomegalovirus infection
⇨ Acyclovir
⇨ Famciclovir
⇨ Ganciclovir
⇨ Trifluridine
⇨ Vidarabine
3) Treatment of HIV infection
⇨ Didanosine
⇨ Stavudine
⇨ Zalcitabine
4) Treament of Covid-19
⇨ Remdesivir
⇨ Nirmatrelvir + Ritonavir
⇨ Baricitinib
⇨ Sotrovinab
Vitamins
Vitamins are organic chemicals that are required for metabolic activities necessary for tissue growth and healing.
Types of Vitamins
1. Fat soluble vitamins⇨ Vitamin A, D, E, K
2. Water soluble vitamins⇨ Vitamin B, C
Vitamins ***
Vit A1: Retinol
Vit A2: Dehydro retinol
Vit B1: Thiamine
Vit B2: Riboflavin
Vit B3: Niacin
Vit B5: Pantothenic acid
Vit B6: Pyridoxine
Vit B7: Biotin
Vit B9: Folic acid
Vit B12: Cyanocobalamin
Vit C: Ascorbic acid
Vit D2: Ergocalciferol
Vit D3: Chole Calciferol
Vit E: Tocopherol
Vit K1: Phytonadionee
Vit K2: Menaquinones
Vit K3: Menadione
Vitamin deficiency disease
Deficiency of Vitamin A
⇨ Night blindness
⇨ Hyperkeratosis
⇨ Keratomalacia
Deficiency of Vitamin B1
⇨ Beriberi
Deficiency of Vitamin B2
⇨ Ariboflavinosis
Deficiency of Vitamin B3
⇨ Pellagra (A disease characterised by skin lesions and mental confusion, primarily caused by a niacin deficiency.)
Deficiency of Vitamin B5
⇨ Alopecia (Deficiency of the hair, which may be caused by failure to grow or loss after growth.)
⇨ Dermatitis
⇨ Paresthesia
Deficiency of Vitamin B6
⇨ Anemia
⇨ Peripheral Neoropathy
Deficiency of Vitamin B7
⇨ Dermatitis
⇨ Enteritis (Inflammation of the intestines, generally the small intestine, that may lead to diarrhea.)
Deficiency of Vitamin B9
⇨ Megaloblastic Anemia
⇨ Birth defect
Deficiency of Vitamin B12
⇨ Megaloblastic anemia
Deficiency of Vitamin C
⇨ Scurvy
Deficiency of Vitamin D
⇨ Rickets
⇨ Oesteomalacia
Deficiency of Vitamin E
⇨ Mild hemolytic anemia in new born infants
Deficiency of Vitamin K
⇨ Bleeding Diathesis
Provitamin
A provitamin is a substance that may be converted within the body to vitamin.
It is the precursor of vitamin.
Example: Provitamin A contain Beta carotine. The body convert beta carotine to retinol
Vaccine
A vaccine is a biological preparation that provides active acquired immunity to a particular disease.
Classification of vaccine
1. Killed (Inactivated) vaccine
2. Live attenuated vaccine
3. Toxoids
Bacterial vaccines
⇨ Cholera
⇨ Plague
⇨ Whooping cough
Viral vaccine
⇨ Hepatitis B vaccine
⇨ Meales
⇨ Mumps
Mechanism of action
Mechanism of Action of Salicylic acid
Salicylic acid
||
Solubilize cell surface protein
||
Keep the stratum cornrum intact
||
Desquamation of keratotic debris
Mechanism of Aspirin as an antiplatelet action
Aspirin
||
Inhibit platelets cyclo-oxygenase
||
Decrease thromboxane A2
||
Inhibit platelets aggregation
||
Prevent thromboembolism
Mechanism of action of Levodopa as an Antiparkinson action
Levodopa
|| < Dopa decarboxylase enzyme
Secretion of dopamine by the action of dopa decarboxylase enzyme
||
Increase dopamine content in basal ganglia
||
Increased activity of dopaminergic system
||
Antiparkinson action
Mechanism of action of Metronidazole
Metronidazole (Antiprotozoal drugs)
||
Enter into anaerobic bacteria & sensitive protozoal cells
||
Reduction of nitro group of metronidazole by Ferredoxin
||
Reduced products react with various intracellular macromolecules (Protein, DNA) of the microorganism
||
Inhibits nucleic acid synthesis and kills the cell of the organisms
Mechanism of action of propranolol as an antianginal action
Propranolol
||
Reduce myocardial contractility
||
Slow the heart rate
||
Reduce cardiac output
||
Decrease cardiac oxygen consumption
Mechanism of action of Aminophylline as an Bronchodilation
Aminophylline
||
Inhibits adenosine phospho-diesterase enzyme
||
Prevent conversion of 3'-5' cAMP to 5' cAMP
||
Increase concentration of 3'-5' cAMP
||
Relaxation of bronchial smooth muscle
||
Bronchodilation
Mechanism of action of Sulbutamol as a Bronchodilation
Sulbutamol
||
Stimulate beta 2 receptor in bronchus
||
Stimulation of adenyl cyclase
||
Conversion of ATP to 3'-5' cAMP
||
Relaxation of bronchial smooth muscle
||
Bronchodilation
Mechanism of action of Ciprofloxacin
Ciprofloxacin (Fluoroquinolones/ DNA gyrase inhibitor)
||
Inhibit DNA gyrase
||
Interfere with the supercoiling of DNA
||
Bacterial death
Mechanism of action of Cephalosporins
Cephalosporins (Cell wall inhibitors/ beta lactam antibiotic)
||
Binds with specific drug receptor on the bacteria
||
Blocking the transpeptidation of peptidoglycans
||
Inhibit the cell wall sysnthesis
||
Activation of autolytic enzyme in the cell wall
||
Bacterial death
Mechanism of action of penicillin
Penicillin (Cell wall inhibitors)
||
Binds to PBPs (Penicillin binding proteins)
||
Inhibition of transpeptidation of peptidoglycan
||
Peptidoglycan synthesis is blocked
||
Cell death
Mechanism of action of Tetracyclines
Tetracyclines (Protein synthesis inhibitor)
||
Enters into the susceptible bacterial cell by two process:
1. By energy dependent active transport
2. By passive diffusion through hydrophillic pores
||
Compete with bacterial tRNA to bind with 30S ribosome
||
Inhibit bacterial protein synthesis
Mechanism of Isoniazide (Antimycobacterial drugs/Treat tuberculosis)
Isoniazide
|| Mycobacterial catalase-peroxidase enzyme
Activated by mycobacterial catalase-peroxidase enzyme
||
Forming a covalent complex with an acyl carrier protein and beta-ketoacyl carrier protein synthesis
||
Blocks the synthesis of mycolic acid
||
Bactericidal effect
* Mechanism of action of Ca++ channel blockers
Ca++ channel blockers
||
Binds with voltage dependent Ca++ channel in depolarized membrane
||
Decrease in trans-membrane Ca++ current
||
Smooth muscle relaxation
* Mechanism of Action of Acetylcholinesterase
Acetylcholinesterase
||
Inhibit cholinesterase enzyme
||
Prevent hydrolysis of acetylcholine
||
Increase acetylcholine concentration
||
Increase acetylcholine activity
Note: Acetylcholine (ACh) is a neurotransmitter, a chemical that carries messages from brain to body through nerve cells.
Note: Cholinesterase enzymes are a group of enzymes that are responsible for the proper functioning of the nervous system. They break down acetylcholine, a chemical that transmits signals across nerve endings. There are two main types of cholinesterase enzymes in the body:
(i) Acetylcholinesterase (AChE)
Found in the brain, lungs, red blood cells, nerve endings, and spleen. AChE is responsible for breaking down acetylcholine into choline and acetic acid, which allows the cholinergic neuron to return to its resting state.
(ii) Butyrylcholinesterase (BuChE)
Also known as pseudocholinesterase, BuChE is found in the liver, serum, heart, pancreas, muscle, and white matter of the brain. BuChE is responsible for processing drugs.
Cholinesterase inhibitors can be used for a variety of purposes, including:
Anesthesia
Treatment of Alzheimer's disease, glaucoma, and myasthenia gravis
Killing insects in pesticides
Chemical warfare agents
Cholinesterase inhibitors can be toxic, and the spectrum of toxicity can vary from patient to patient. The most recognized form of toxicity is SLUDGE syndrome, and severe respiratory depression can also occur.
* Mechanism of Action of Proton pump inhibitor
Proton pump inhibitor (PPI)
||
Interfere in the final stage of gastric acid production by blocking/ forming a covalent bond to two sites of the H+/K+, ATPase enzyme system at the secretory surface of the gastric parietal cell.
||
This lead to inhibition of both basal & stimulated gastric acid secretion irrespective of the stimulus.
* Mechanism of Antacid
Antacids
||
Acts with HCl and neutralizes it
||
Raise of pH (3.5) and pepsin become inactive
||
Protect the gastric mucosa
||
Healing ulcer
Note: Pepsin is a stomach enzyme that serves to digest proteins found in ingested food. Gastric chief cells secrete pepsin as an inactive zymogen called pepsinogen. Parietal cells within the stomach lining secrete hydrochloric acid that lowers the pH of the stomach. A low pH (1.5 to 2) activates pepsin.
Note: HCl is produced by the parietal cells of the stomach. To begin with, water (H2O) and carbon dioxide (CO2) combine within the parietal cell cytoplasm to produce carbonic acid (H2CO3), which is catalysed by carbonic anhydrase. Carbonic acid then spontaneously dissociates into a hydrogen ion (H+) and a bicarbonate ion (HCO3–).
The hydrogen ion that is formed is transported into the stomach lumen via the H+– K+ ATPase ion pump. This pump uses ATP as an energy source to exchange potassium ions into the parietal cells of the stomach with H+ ions.
The bicarbonate ion is transported out of the cell into the blood via a transporter protein called anion exchanger which transports the bicarbonate ion out the cell in exchange for a chloride ion (Cl–). This chloride ion is then transported into the stomach lumen via a chloride channel.
This results in both hydrogen and chloride ions being present within the stomach lumen. Their opposing charges leads to them associating with each other to form hydrochloric acid (HCl).
* Mechanism of NSAID
Membrane phospholipids
|| Phospholipase enzyme
Produce arachidonic acid by the action of enzyme NSAID
.......... || (-) NSAID
Produce Cyclo-oxygenase enzyme (COX)
.......... ||
Produce COX I and COX II enzyme
COX-I (Constitutive enzyme) || COX-II (Inducible enzyme)
Produce protaglandin ....... || Produce Prostaglandin
Give Renal function, Platelet function, Gastric mucosal protection ||Smooth muscle contraction, Fever, Pain & Inflammation
* Mechanism of H2 Blocker
H2 Blocker
||
Competitively block the H2 receptor
||
Histamine cannot acts on H2 receptor
||
Decrease cAMP ( Cyclic Adenosine Monophosphate)
||
Reduction of HCl Secretion
||
Healing of ulcer
Note: Histamine is a signaling molecule that plays a key role in allergic reactions. It's released from white blood cells during allergic reactions, causing blood vessels to dilate and become leaky, which can lead to swelling.
Note: Cyclic adenosine monophosphate (cAMP) is a second messenger used for intracellular signal induction. It is synthesized from adenosine triphosphate (ATP) by enzymes (g-proteins) that are attached to metabotropic receptors and become released when the receptor is activated.
* M/A of Benzodiazepam
Benzodiazepam
||
Binds with specific regulatory site on the GABA receptor in the brain (Gama amino butyric acid)
||
Enhance of GABA activity
||
Opening Cl- channels
||
Hyperpolarization of cells
||
Depression of CNS
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