All Mechanism Of Action And Classification Drugs

E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

Adverse Drug Effects Introduction-Classification-Categorization Concept & Idea by- Solution Pharmacy E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

Drug/ Medicine

Drug is a chemical moiety (either natural or synthetic) which is used for the prevention, diagnosis and treatment of any disease or disorder. Disease is caused by microorganism mainly and disorders And Disorders are result of imbalance of various biochemicals within body itself.

Adverse Effect

Any effect produced by the drug which is not expected or not desired and unintended is called adverse drug effects. It is one of the broad definitions which cover many subtypes from simple to serious effects.

Disease Disorder

Diagnosis

Treatment

Drug/Medicine E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

Desirable Effects Desirable effect means all those effect produced by drug which we are expecting and willing to get.

Undesirable Effects All those effect given by drug which is not good for us and it may cause simple to dangerous effect.

Example Paracetamol, Nimesulide, Ibuprofen,

Aspirin,

Indomethacin Aspirin

Different Categories

Predicted

NSAIDS Non Steroidal Anti-inflammatory Drugs

Unpredicted

Type A or Augmented

Side Effects

Type B or Bizarre

Rashes, Etching

Secondary Effects Suspension of bacterial flora

Analgesic Effect Reduce pain by inhibiting PG synthesis and increasing pain threshold potential.

Antipyretic Effect Reduce fever by controlling thermoregulatory center in brain

Toxic Effects- Poisoning Intolerance Drug Allergy- Humoral & Cell Mediated Photosensitivity- Phototoxic and Photo allergic Drug Dependence Physiological-Physical-Drug Abuse-Drug Addiction-Drug Habituation

Anti-Inflammatory Effects Drug Withdrawal reaction- Alcohol and LSD Reduce inflammation by inhibiting COX-I and COXII

Teratogenicity- Thalidomide Mutagenisity or Carcinogenicity Drug Induced Disease- Peptic Ulcer by NSAIDS

E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

Antianginal Drugs Classification & Mechanism of Action Based on KD Tripathi

Angina is a chest pain or we can say that it is a signal informing us that there is lack of oxygen supply to myocardium. This is generally occurring at the left side of the chest. It has 02 main types- (1) Classical Angina (Common form) - Those type of angina which may arise due to over work like- exercise, emotion etc. (2) Variant or prinzmetal’s Angina (uncommon form) - Attack occurs at rest or during sleep and doesn’t disappear after rest.

Nitrates

Beta Blocker Propranolol, Metoprolol, Atenolol, and others

Short Acting Glyceryl Trinitrate (GTN, Nitro Glycerin)

Long Acting

Ca+ Channel Blocker

K+ Channel Opener

Others

Nicorandil

Dipyridamole, Trimetazidine, Ranolazine, Oxyphedrine

Phenyl alkylamineVerapamil, BenzothiazepineDiltiazem, DihydropyridinesNifedipin, Felodipine, Amlodipine, Nitrendipine, Nimodipine, Lacidipine, Lercanidipine, Benidipine

Isosorbide dinitrate, Isosorbide mononitrate, Erythrityl tetranitrate Pentaerythritol tetranitrate

Other Clinical Application of K+ Channel Opener 1. 2. 3. 4. 5. 6. 7.

Angina Pectoris Hypertension Congestive heart failure Myocardial salvage in MI Alopecia Bronchial asthma Urinary urge incontinence 8. Premature labour (Ref- KD Tripathi)

www.facebook.com/pharmavideo/

E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

Antiarryhythmics Drugs Classification and Mechanism of Action

Class- I

Class- II

+

Class- III +

Class- IV +

Na channel blocker

B adrenoreceptor

K channel blocker

Ca channel blocker

Disopyramide, Flecainide Lidocaine, Mexiletine Procainamide, Propafenone, Quinidine

Atenolol, Esmolol, Metoprolol

Amiodarone, Dofetilide, Dronedarone, Ibutilide, Sotalol

Diltiazem, Verapamil

Adenosine, Digoxin, Magnesium sulfate

Causes of Arrhythmia 1. Abnormal Automaticity- SA node shows the fastest rate of phase 4 depolarization and therefore, exhibits a higher rate of discharge than that occurring in other pacemaker cells exhibiting automaticity

Nerve Impulse

Normal Conduction

Other Antiarrythmic Drugs

Unidirectional Block

2. Abnormality in impulse conduction- Impulse from higher pacemaker centers are normally conducted down pathways that bifurcate o activate the entire ventricular surface. A phenomenon is called reentry may occur if unidirectional block occurs. Reference- Lippincott (Pharmacology) 6th Edition

Ventricle Wall

Block

E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

Anti Microbial Drugs Classification According to Mechanism of Action Classification Reference- KD Tripathi (Pharmacology)

Inhibit Cell wall synthesis

Cause Leakage From cell membrane

Penicillin

Polymyxines

Cephalosporins

Colistin

Cycloserine

Nystatin

Cloramphenicol

Bacitracin polymers Amphotericin- B

Erythromycin

Bacitracin

Inhibit Protein Synthesis

Cause misreading or RNA and affect permeability

Inhibit DNA gyrase

Interfere with DNA function

Interfere with DNA synthesis

Tetracycline

Aminoglycosides Streptomycin Gentamycin

Fluoroquinolones Ciprofloxacin etc

Rifampin Metronidazole

Acyclovir Zidovudine

Sulfonamides, PAS, Sulfones, Trimethoprim, Ethambutol,

Interfere with Intermediary Metabolism

Clindamycin

Vancomycin

Hamycin

Linezolid www.facebook.com/pharmavideo/

Note- Mnemonics are based on my thoughts; it may or may not useful to you. It’s always better to create your own so you may memorize it. E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

Anti Microbial Drugs Classification According to Various Parameters Classification Reference- KD Tripathi (Pharmacology)

Types of Organism Against which primarily Active

Spectrum of Activity

Antibacterial Penicillins, Aminoglycosides Erythromycin etc

Type of Activity

Bacteriostatic

Bacteriosidal Penicillin

Narrow Spectrum

Broad Spectrum

Sulfonamide

Penicillin G

Tetracycline

Tetracycline

Antifungal Griseofulvin, Amphotericin B, Ketoconazole etc

Antiviral

Streptomycin

Acyclovir, Amantadine, Zidovudine etc

Erythromycin

Antiprotozoal Chloroquine, Pyrimethamine, Metronidazole, Diloxanide etc

Chloramphenicol

Chloramphenicol Erythromycin Ethambutol Linezolid

Aminoglycosides Polypeptides Rifampin Isoniazide Pyrazinamide Cephalosporin

Anthalmentic Mebendazole, Pyrantel, Niclosamide, Diethyl carbamazine etc

Vancomycin Nalidixic Acid Ciprofloxacin Metronidazole Cotrimoxazole

E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

Antihistamine Drug

H1 Blocker

H2 Blocker

H3 Blocker

H4 Blocker

Conventional Antihistaminic

Highly Sedative

Moderately Sedative

Mild Sedative

Diphenhydramine, Dimenhydrinate, Promethazine, Hydroxyzine

Pheniramine, Cyproheptadine, Meclizine, Buclizine, Cinnarizine

Chlorpheniramine, Dexchlorpheniramine, Dimethindene, Triprolidine, Mebhydroline, Cyclizine

2nd Generation

Fexofenadine, Loratadine, Desloratadine, Cetirigine, Levocetrizine, Azelastine, Mizolastine, Ebastine, Rupatadine

Pharmacological Action

1

Antagonism of Histamine – Reverse Histamine induced bronchoconstriction, Intestinal and other smooth muscle contraction

2

Antiallergic Action – Suppress type I Hypersensitivity reaction. Urticaria, itching and angioedema are well controlled.

3

CNS – Few of them depress CNS. Few are effective in preventing motion sickness. Few reduce tremor, Rigidity, antitussive

4

Local anesthetics – Some antihistaminic are strong and some are having weak membrane stabilizing property.

5

Blood Pressure- Most antihistaminic drug cause fall in BP on IV injection.

Diagrams and explainations are made by solution-pharmacy to make you better understand.

E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

Classification and Mechanism of Action for Antihistamine Drug Key Point to Understand- ‘Histamine’ is made up of two simple words- Histo (Tissue) + Amine. If we add them together the meaningful sentence will be- Amine released from tissue. Histamine is stored and release from mast cells. Other tissue like- Skin, gastric and intestinal mucosa, lungs, liver and placenta. Histamine receptors are of basically 02 types- (1) H1 and H2. H3 is also available. Histamine initiate allergic reaction thus antihistaminic drugs give relief from allergy by blocking any of the histamine receptor.

Antihistamine Drug

H1 Blocker

H2 Blocker

H3 Blocker

H4 Blocker

H2 Antihistaminic Cimetidine, Ranitidine, Famotidine, Roxatidine

H2 Receptor antagonist and regulation of gastric acid secretion Gastric acid (Hcl) is secreted by the parietal cells from the mucosa of gastrointestinal tract, and that is stimulated by acetylcholine, histamine, and gastrin. The receptor medicated binding of acetylcholine, histamine, and gastrin result into activation of protein kinase which ultimately stimulate the H+/K+ ATP. Thus it is very simple that if someone is willing to inhibit the release of gastric acid he or she has to inhibit the binding of any of the above agent to their respective receptor. So the H2 Receptor antagonist doesn’t allow the agent to bind to the receptor and inhibit the release of gastric acid.

Histamine Blocker

Acetylcholine

Histamine

Gastrin

Gastric Acid secretion stimulation Diagrams and explainations are made by solution-pharmacy to make you better understand.

E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

Anti-Hypertensive Drugs Prevention is always better than cure Classification- KD Tripathi 5

1

2

3

4

Diuretics

ACE Inhibitor

Angiotensin Blocker

Calcium Channel Blocker

6

Beta+Alfa Blocker

Beta Blocker

Examples of above listed Class

7

8

Alfa Blocker

Central Sympatholytics

9

Vasodilator

Channel is closed

Thiazide Diuretics

Channel is Open Increase Water & Sodium Excretion

Thiazide- Hydrochlorothiazide, Chlorthiazide, Indapamide High Ceiling- Furosemide K+ Sparing- Spironelactone, Amiloride

Captopril, Enalapril, Linsopril, Perindopril, Ramipril, Fosinopril etc.

Losartan, Candesartan, Irbesartan, Valsartan, Telmisartan

Verapamil, Diltiazem, Nifedipin, Felodipine, Amlodipine, Lacidipine

Short Term Effect

Long Term Effect

Open Sodium content in cell Decrease Blood Volume Channel isDecrease

Calcium channel Blocker

Decrease Muscles sensitivity to vasopresser

Decrease cardiac output

04

Decrease Peripheral Resistance Propranolol, Metoprolol, Atenolol

Increase

01

Labetalol, Carvedilol

Heart rate Contractility Conduction

Decrease Blood Pressure

Beta Receptor Blocker Prazocin, Terazocin, Doxazosin, Phentolamine, Phenoxybenzamine

Decrease output of Symp. Nervous system

Renin from Kidney Clonidine, Methyldopa

Arteriolar- Hydralazine, Minoxidil, Diazoxide Arteriolar+ Venous- Sodium Nitropruside

All diagrams and design- Solution-Pharmacy

05

Angiotensinogen

Angiotensin I (Inactive)

Increase vasodilatation of vascular muscle

Angiotensin II

ACE Inhibitors

Decrease sod. And water retention

Aldosterone Production

Angiotensin Blockers

02

Blood Pressure

03

www.facebook.com/pharmavideo/

ANTIVIRAL DRUG Classification and Mechanism of Action

Anti-Herpes Virus Idoxuridine, Trifluridine, Acyclovir, Valacyclovir, Famciclovir, Ganciclovir, Valganciclovir, Cidofovir, Foscarnet,, Fomivirsen

Anti-Influenza Virus Amantadine, Rimantadine, Oseltamivir, Zanamavir

Anti-Hepatitis virus or Nonselective antiviral drugs

Anti-Retrovirus

Primarily for Hepatitis B Lamivudine, Adefovir, Dipivoxil, Tenofovir Primarily for Hepatitis C, Ribavirin, Interferon Alpha

Nucleoside reverse transcriptase Inhibitors (NRTIs) Zidovudine (AZT), Didanosine, Stavudine, Lamivudine, Abacavir, Emtricitabine, Tenofovir, (Nt RTI)

Non Nucleoside Reverse transcriptase Inhibitors (NNRTIs) Nevirapine, Efavirenz, Delavirdine

Protease Inhibitors Ritonavir Atazanavir, Indinavir, Nelfinavir, Saquinavir, Amprenavir, Lopinavir

Entry (Fusion) Inhibitor Enfuvirtide

CCR5 Receptor Inhibitor Maraviroc

Integrase Inhibitor- Raltegravir

E Mail- [email protected] &

Viral Reach solution at- www.facebook.com/pharmavideo/ fusion with host cell

1

Fusion Inhibitor

Budding (Viral release)

Virus

2 Penetration

Enfurvirtide (HIV)

3

Mature Virus Neuraminidase Inhibitor

8

Interferon-Alfa (HBV, HCV)

Un-Coating

7

Packaging and Assembling

Amantadine Rimantadine (Influenza) Viral Protein

Viral RNA 4

Reverse transcription

Protease Inhibitors

Translation Viral genomic mRNA Viral mRNA

Reverse Transcriptase Inhibitor

Viral DNA

Transcription

Host DNA

6

Transcription

Integrase

Cytoplasm

Nucleus

E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

5

Integration of Host DNA with Viral DNA

Integrase

Inhibitors

7

Viral fusion

Penetration

1

Herpes Virus

Mature Virus

E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

with host cell

Budding (Viral release)

6

Host cell

Packaging and Assembling of virion 5

2

Viral Protein

Translation

Uncoating

Host DNA Viral mRNA

Viral DNA

Viral mRNA

3

Acyclovir, Foscarnet, Ganciclovir

Inhibition of Viral DNA polymerase

4

×

Synthesis of viral DNA New viral DNA

Nucleus

Cytoplasm

Anti- herpes drug’s mechanism of action E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

Classification, Mechanism of Action and Tricks for

Drugs for Cough Classification- KD Tripathi

A

B

C

Pharyngeal Demulcents

Expectorants /Mucokinetics

Lozenges, Cough Drops, Linctuses Syrup, Glycerin, Liquorice

Those which helps to Expel the cough. or which increase the kinetic movement of cough

www.facebook.com/pharmavideo/ Mechanism of Action Bronchial secretion enhancer

Mucolytics

D

Antitussive Cough center suppressers Drug which decrease sensitivity of cough center.

Adjuvant Antitussive Bronchodilators, Salbutamol, terbutaline

www.facebook.com/pharmavideo/ Mechanism of Action Example of the Class

Example of the Class

Sodium citrate, Potassium citrate, Potassium Iodide, Guaiphenesin, Balsum of tolu, Vasaka, Ammonium Chloride. सेक्रेशन पे प्रभाव पड़ेगा इससे गले से बेहतर वोइस आनी चालू होगी Bromhexine, Ambroxole ,Acetyl cysteine

Opioids Non Opioids Antihistaminic

Codeine, Pholcodeine कफ को फे क दो Noscapine, Dextromethorphan, Chlophedianol नहीं देना चोकलेट कफ में Chlorpheniramine, Diphenhydramine, Promethazine. चलो डटट को प्रप्रवेंट करें ( Asthma is related with dust)

Carbocisteine, बैठा आवाज अब चालू हो जाएगा

Key points- Coughing is a protective phenomenon until it does not hurt or create uneasiness. Cough is a protective reflex which tries to expel or eliminate the unwanted particles from our air passage along with mucus and other watery substances. The arising of cough is from stimulation of mechano or chemoreceptor present in throat, respiratory passage or in any other associated part of lungs. The main objectives of using anti cough drugs are to reduce the viscosity of cough so that they may be easy expelled. And this may achieve by breaking the bond between cough mucus which are used to bind them together. A Mechanism

Distance in bond (Less viscous)

Demulcents Closely bond (More Viscous)

Irritant

Mucus

Expectorants

B Mechanism

Viscosity of mucus Due to bond between them

Demulcents sooth the irritant www.facebook.com/pharmavideo/

www.facebook.com/pharmavideo/ Expectorant or Mucokinetics are the drugs which produce their action either by increasing mucus production or by decreasing the viscosity of fluid so they become thin and easily expelled out.

Demulcent sooth and cover the irritant and the stimulus released by irritant. This is not a treatment; this is just a temporary relief.

Opioids increase cough threshold

Cough Center

Histamine

01

Activate

Mast Cells

Cough Start

Ag Binding sites

Low threshold Irritant

Reduce tussal impulse

02 Allergens C Mechanism

Antitussive www.facebook.com/pharmavideo/

Antitussive are the agent or drug which generally increase the threshold of cough center, or reduce the tussal impulse or act by both mechanism.

Mechanism of Action

* All Diagrams (Except Brain) and explanations are made by solution pharmacy Note- All mechanisms of action are converted into diagram by Solution-Pharmacy. These are not available elsewhere

Cough Activation Many H1 antihistaminic drugs showed their role as Antitussive agent. They produced antitussive action due to Their sedative and anticholinergic action, but lack selectivity for cough center.

* Diagrams Except brain) is made by solution to make you better understand

C Mechanism

E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

Drugs for Constipation Classification based on KD Tripathi (Pharmacology)

Bulk Forming Agents

Stool

Stimulant

Osmotic

Softener

Purgative

Purgative

Example

Example

Bran

Docusates (DOSS)

Diphenylmethanes

Magnesium Salt

Phenolphthalein, Bisacodyl Sodium picosulfate

Sulfate, Hydroxide

Antraquinones

Sulfate, Phosphate, SodiumPotassium tartrate, Lactose

Sodium Salt

Psyllium (Plantago)

Liquid Paraffin

Senna, Cascara Sagrada

Ispaghula

5HT4 Agonist Mechanism of Action

Tegaseroid Water

Osmosis

Methyl Cellulose

Fixed Oil Castor Oil

Intestine Mechanism of Action

Mechanism of Action

* Mechanism of Action- Representation by Solution Pharmacy Key point- Constipation is not a single disease or disorder; it is a root cause for several GIT related problems. When there is lack of water in large intestine and lack of fiber intake in diet, constipation take place. Constipation’s treatment lies within the problem itself. Target for the treatment include1. Increase amount of water inside intestine 2. Increase fibers content in diet 3. Increase expel of stools by increasing peristaltic movement 4. Stimulating or irritating the colon to force the evacuation of stools 5. Increase retention of sufficient water inside intestine *Based on our concept. Reference not available E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

Diabetes Mellitus (DM) Introduction to basic Points Classification- KD Tripathi

TYPE- I Diabetes Mellitus Insulin Dependent Juvenile onset D. Mellitus

TYPE- II Diabetes Mellitus Non Insulin Dependent Maturity onset Juvenile DM

www.facebook.com/pharmavideo/

www.facebook.com/pharmavideo/

As name indicate “Insulin Dependent” that means body is dependent on Insulin from outside source, because body’s Insulin production center (beta cell in Pancreases) is destroyed due to any reason. And if there is no Functional beta cell available so how Insulin will be made, that’s why we take Insulin to manage deficiency.

In case of Non Insulin dependent diabetes mellitus the situation is not same as “Insulin Dependent” because the Insulin production center is get weakened but not destroyed, so if we try to make that center healthier our problem will be solved. There is one more reason that isInsulin is in appropriate amount but there is some resistance to its binding to Insulin receptor.

* Diagrams are Made by solution to make you better understand

Profile

Insulin Dependent Body is not in condition to make sufficient Insulin Destruction of Beta cell

Body can make sufficient Insulin

Cause

Autoimmune disorder

(1) Abnormality of gluco-receptor (2) Reduced sensitivity of peripheral tissue for Insulin (3) Excess of hyperglycemic hormones

Treatment

Insulin from external sources

Oral hypo glycaemic Drugs

Insulin production Status of Beta cell

Non Insulin Dependent

No loss or Destruction of Beta cell

www.facebook.com/pharmavideo/

Non Insulin Dependent

Diabetes Mellitus (DM)

Improve Insulin Availability Exogenous Insulin Sulfonylureas Meglitinide/Phenylalanine analogus

Overcome Insulin Resistance Biguanides Thiazolidinediones Alfa-Glucosidase Inhibitors

FOOD Containing Glucose Beta Cell

Type I

Pancreases- Insulin

Diabetes Mellitus

Destroy

Glucose

Type II

Diabetes Mellitus Create resistance In Insulin binding to receptor

Utilized by Cell for various Activity

(1) In absence of Insulin unused glucose is stored in blood and excreted in urine (2) Increase blood sugar increase osmotic difference and demand more water (Trust) (3) Excess sugar in tiny capillary may obstruct eye’s vessels (4) Unavailability of glucose in cell cause weakness

E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

Reference- Lippincott Pharmacology

Hypothalamus

Growth hormone Releasing hormone

Corticotropin Releasing hormone

Anterior Pituitary Gland

Throtropin Releasing hormone

Gonadotropin Releasing hormone

Prolactin Inhibiting hormone

Prolactin Releasing hormone

Flow Chart by- Solution Pharmacy E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

Throtropin Follicle Stimulating hormone Stimulating hormone

Growth hormone

Adrenocorticotropic Hormone

Lever

Adrenal Cortex

Thyroid

Insulin like growth factor

Glucocorticoids, Mineralocorticoids, Androgens

Thyroxin

Ovary

Estrogen

Luteinizing Hormone (Female)

Ovary

Progesterone

Luteinizing Hormone (Male)

Testis

Prolactin

Brest

Testosterone

Summarized Flow Chart- Hypothalamic and Anterior Pituitary Hormones

Immunity

Immunology Immunology is made of Immune + logy = Immunology. That means the complete study of Immune (Our body’s bodyguard) system which majorly include antigen and antibody and their interaction, resulting in desirable or undesirable biological action. Reference- NK Jain (Microbiology)

Natural Immunity

Species

Racial

Species Man is susceptible for plague but not fowls. Mice are not affected by typhoid fever but man suffers.

Acquired Immunity

Individual

Active

Natural/Clinical Subclinical

Passive

Artificial

Natural

Artificial

Vaccine- Dead or Extract attenuated Toxoids

Congenital Colostrums

Antiserum Antitoxin

Race Negroes possess high resistance to yellow fever than white man. Negroes and white Indian are more susceptible to TB than Caucasian race.

Individuals Children of age-2-5 are susceptible to diphtheria whereas most adult are immune to it.

Natural It acquires when a person recover from- diphtheria, small pox and poliomyelitis. A person become immune because it’s his antibody producing cell has received an adequate stimulus.

Natural Acquired Immunity Antibody formed in a mother in response to disease may be transferred to fetus through the placental blood.

Artificially Acquired Immunity

Artificial This is acquired by the administration of antigen usually by injection. Example- Vaccine either live or dead.

This is acquired by injecting the preparation known s antiserum. These are the Antibodies produced in animal.

E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

Principle & Mechanism of Drug Action (Pharmacodynamic)

Mechanism of Drug Action

Irritation Example- Counter Irritant like- drugs for constipation

Bulk Laxative

Physical Other Mechanism

Main Mechanism

Depression Example- Barbiturate depresses CNS, Quinidine depresses heart, and Omeprazole depress gastric acid secretion.

Replacement Example- Levodopa in Parkinson’s, Insulin in diabetes and Iron in Anemia.

Principle of Drug Action

Stimulation Example- Adrenaline. Stimulates heart, pilocarpine stimulates salivary glands.

Chemical

Antacid neutralize acid by its basic nature

Enzyme

Inhibitor

Substrate NO Product

www.facebook.com/pharmavideo/

Close

Inhibitor

Product

Competitive Agonist

RECEPTOR

Instagram

Receptor

Open

Modulator

Agonist

Facebook

Transporter Ions

Substrate

Cytotoxic Selective Cytotoxic action on invading parasite or cancer cell without affecting host cell. Example- Penicillin, Chloroquine, Zidovudine, cyclophosphamide.

Ion Chanel

www.facebook.com/pharmavideo/ 00 km

Transducer

Action

Classification and Mechanism of Action

NSAID Non steroidal anti-inflammatory Drugs *Classification- KD Tripathi

Non-Selective

Preferential

Selective

Analgesic-Antipyretic

COX Inhibitor

COX2 Inhibitor

COX2 Inhibitor

Anti-inflammatory

Nimesulide, Diclofenac, Aceclofenac, Meloxicam, Etodolac

Celecoxib, Etoricoxib, Parecoxib

Action

Category Salicylates Propionic acid derivative Fenamate Enolic acid derivative Acetic acid derivative Pyrazolone derivative

Example Aspirin Ibuproprofen, Naproxen, Ketoprofen, Flurbiprofen Mephenmic acid www.facebook.com/pharmavideo/ Piroxicam, Tenoxicam Ketorolac, Indomethacin, Nabumetone Phenylbutazone, Oxyphenbutazone

with poor

Example Paracetamol (Acetaminophen) Metamizol, Propiphenazone Nefopam *Constitutive = Constant Production

Key Point (Solution) - As name Indicate NSAIDs are those agents which are used to get relief from pain, inflammation and fever. And as per the COX pathway we understand that COX-1 and COX-2 ultimately form prostaglandin which initiates perception of pain and inflammation. So anyhow if we block or inhibit the synthesis of PG we may reduce pain and inflammation. Although COX-1 is constitutive in nature thus it always get secreted without induction of injury and called as a house keeper so it’s better to inhibit COX-2 rather than COX-1.

* Tissue Injury (Applicable for COX-2)

Breakdown of Membrane Phospholipids Arachidonic acid

Mechanism of Action Cyclooxygenase Pathway *Rough Idea- Lippincott

COX-1 perform housekeeping function Like neutralizing gastric acids

Inhibit

COX-2 gene transcription COX-1 gene transcription

Induced byOxidative Stress, Injury, Ischemia, Seizures

Glucocorticoids

www.facebook.com/pharmavideo/

Inhibit

mRNA

mRNA

Selective Non-Selective

COX Inhibitor

Inhibit Non-Selective

Inhibit

COX Inhibitor COX- 1

COX-2Inhibitor

Side Effect- Gastric Ulcer

Celecoxib, Etoricoxib, Parecoxib

Inhibit

COX- 2

PROSTAGLANDIN *Diagrams and explainations are made by solution-pharmacy S E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

Antiparkinsonian Drugs

Drug affecting brain dopaminergic system

Classification- KD Tripathi

Drug affecting brain cholinergic system

Dopamine Precursor

Central Anticholinergic

Levodopa

Trihexyphenidyl, Procyclidine, Biperiden

Peripheral decarboxylase inhibitor Crbidopa, Benserazide

“ACLBSEBRPT” Acetylcholine Level Badalne Se Brain Rog Parkinson Taklif deta hai. Acetylcholine लेवल बदलने से ब्रेन ब्रेन रोग पार्किन्सन तिलीफ देता है

Antihistaminic Orphenadrine, Promethazine

Dopaminergic Agonist Bromocriptine, Ropinirole, Pramipexole

Parkinsonism

www.facebook.com/pharmavideo/

MAO- B Inhibitor Selegiline

Dopamine

COMT Inhibitor Entacapone, Tolcapone

Dopamine Facilitators

Acetylcholine

Imbalance between Acetylcholine and Dopamine

Amantadine

Parkinsonism is an extra pyramidal motor disorder, symptoms includes- rigidity, tremors, with defective gesture and posture. Parkinsonism is a result of imbalance between acetylcholine and dopamine. When there is remarkably decrease in dopamine level or increase in acetylcholine level, Parkinsonism take place. As cause is clear their treatment is also very clear. Treatment goal is to restore the balance between above said neurotransmitters either by increasing dopamine by eternal source or by decreasing the level of acetylcholine. E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

DRUG USED FOR PEPTIC ULCER Based on KD Tripathi Classification

Reduction of Gastric acid Secretion

Neutralization of Gastric acid

Ulcer Protective

H2 Antihistaminic Cimetidine, Ranitidine, Famotidine, Roxatidine

Systemic

Example

Sodium bicarbonate, Sodium citrate

Sucralfate, Colloidal bismuth sub citrate

Proton Pump Inhibitor

MgOH, Magnesium trisilicate, Aluminum hydroxide gel, Magaldrate, Calcium carbonate

Anti H Pylori Drugs

Example Amoxicillin, Clarithromycin Metronidazole, Tinidazole Tetracycline

No systemic Omeprazole, Esomeprazole, Lansoprazole, Pantoprazole, Rabeprazole, Dexrabeprazole

NaHCO3+HCL

NaCl+H2O+CO2

Base

Pylori

Anticholinergic Drugs Pirenzepine, Propantheline, Oxyphenonium

Antibiotics

Acid + Base

Prostaglandin Analogue Misoprostol

Anti Pylori Ulcer Neutralization

Coating

Diagram Idea- Lippincott Pharmacology

Key point- Peptic ulcer is result of imbalance between attacking gastric acid and protective bicarbonate system. Gastric acid secretion is regulated by cholinergic system, Histaminic system, stress, Hyperacidity, Microorganism and somehow smoking and spicy diet. The first attempt towards treatment is neutralization of hyper acidity by using antacids which are chemically base and they give their action by neutralizing acid. Protective drug are not the treatment they can mask the pain or irritation signal arising from the ulcer. Anti microbial drug may only be effective in case of infection. * Diagram Idea and Designing concept by- Solution Pharmacy- www.facebook.com/pharmavideo/

E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

PHARMACOLOGY Study of Pharmacokinetics and Pharmacodynamic profile

Trick- In Pharmacodynamic & Pharmacokinetics ‘Pharmaco’ word is common. And now in Dynamic the 1st word is D and in Drug the first word is also D so Dynamic is related to Drugs.

Pharmacodynamic What does drug do to the body?

Pharmacokinetics What does body do to the drug?

We take drugs because we are havingA

Diseases Caused by External Substance

Disorder s Caused by

D A

M

E

Absorption of medicine from their site of administration to produce response.

Imbalance of internal biochemical

What happens when we take those drugs/medicines? Distribute throughout the body after absorption

Desired Effects Diagnosed

Undesired Effects Prevention

Treatment

Side Effect

Adverse Effect

Toxic Effect

Fatal Effect Vaccine Bismuth Sulphate

Unwanted and toxic substance get excreted viaurine, stool, sperm, gas etc

Extension of ADR Paracetamol- Reduce fever (Temperature) Antacids- Reduce Acidity (Neutralization) Penicillin- Prevention from Infections

Fluorescence X-Ray

Metabolism breakdown complex molecules to small molecules that it may be used

These are examples of what DRUGS are doing to the BODY

Side Effects- fatigue, nausea, vomiting, decreased blood cell counts, hair loss, and mouth sores. Adverse Effects- stomach irritation and bleeding often occur in people who regularly use aspirin or other nonsteroidal anti-inflammatory drugs (NSAIDs)

E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

Antirheumatoid Drugs Classification- KD Tripathi

Disease Modifying AR Drugs

Biological Response Modifier

Adjuvant Drugs

Etanercept Infliximab, Adalimumab, Anakinra

Corticosteroids Prednisolone and others

Immunosuppressant(Methotrexate, Azathioprine, Cyclosporine) Sulfasalazine, Chloroquine, Leflunomide, Gold sod. Thiomalate, Auranofin, d-Penicillamine

www.facebook.com/pharmavideo/

Key point- Antirheumatoid arthritis (RA) is an autoimmune disease In RA there is joint inflammation, synovial proliferation and destruction of articular cartilage. These inflammatory cells secrete lysosomal enzyme which damage cartilage and erode bone, while PG produced in the process cause vasodilatation and pain.

2 ATP + CO2 + Glutamine

Carbamoyl Phosphate

Dihydroorotate NAD+ Dihydroorotate

2 ADP + Pi + Glutamate

NADH + H+

Dehydrogenase

Orotate www.facebook.com/pharmavideo/

Orotidine 5’ Monophosphate OMP

Mechanism of Action Leflunomide is an immunomodulatory

agent that preferentially cause fully arrest of the autoimmune

Uridine 5’ Monophosphate

lymphocytes through its action on Dihydroorotate Dehydrogenase.

DNA-RNA

Purine

Anti- Gout Drugs

Hypoxanthine Allopurinol

Xanthine Oxidase

Febuxostat

Xanthine

For Acute Gout

For Chronic Gout

Allopurinol

Febuxostat

Xanthine Oxidase

NSAID,

Colchicine, Corticosteroids

Uric Acid Uric Acid

Uricosurics Synthesis Inhibitor Probenecid, Sulfinpyrazone, Allopurinol, Febuxostat

Phagocytosis of uric acid crystal by neutrophils

www.facebook.com/pharmavideo/

Hydrolytic enzyme Lysosome

Neutrophil Leukotriene Releases

Colchicine

Rupture of Lysosome, followed by death of phagocyte & release of hydrolytic enzyme

Acute Inflammation Diagrams and explainations are made by solution-pharmacy to make you better understand

E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

SEDATIVE - HYPNOTICS These drugs make exited patient calm and cool with and without causing sleep. They are differ only in concentration

Classification- KD Tripathi

SEDATIVE

D T F N A

दिमाग ठं डा रखने से फटाफट नींि आती है

Sedative are those drugs which make patient calm and relax without causing sleep, although patient may feel dizziness and may loss alertness or responsiveness.

L O D A C

लो डराने आ गया क्लाससदफके शन C

C

D

L

चलो चले िवाई लेने एंटी कनवलसन का

E Mail- [email protected] Reach solution at- www.facebook.com/pharmavideo/

𝐁𝐞𝐧𝐳𝐨𝐝𝐢𝐚𝐳𝐞𝐩𝐢𝐧𝐞

𝐒𝐡𝐨𝐫𝐭 𝐀𝐜𝐭𝐢𝐧𝐠 Butobarbitone Phenobarbitone

𝐍𝐞𝐰𝐞𝐫 𝐍𝐨𝐧 𝐁𝐙𝐃 𝐇𝐲𝐩𝐧𝐨𝐭𝐢𝐜𝐬 Zopiclone, Zolpidem, Zaleplon

𝐔𝐥𝐭𝐫𝐚 𝐒𝐡𝐨𝐫𝐭 𝐀𝐜𝐭𝐢𝐧𝐠 Thiopentone Methohexitone

𝑺𝒕𝒂𝒈𝒆 − 𝟎

𝑨𝒘𝒂𝒌𝒆

𝐶𝑜𝑛𝑠𝑡𝑖𝑡𝑢𝑡𝑒 1 − 2%

Reach solution at- www.facebook.com/pharmavideo/

Hypnotic Diazepam Temazepam Flurazepam Nitrazepam Alprazolam

Antianxiety Lorazepam Oxazepam Diazepam Alprazolam Chlordiazepoxide

दिमाग ठं डा रखने से फटाफट नींि आती है

लो डराने आ गया क्लाससदफके शन

Anticonvulsant Clonazepam Clobazam Diazepam Lorazepam

𝑺𝒕𝒂𝒈𝒆 − 𝟎𝟏

𝑫𝒐𝒛𝒊𝒏𝒈

𝐶𝑜𝑛𝑠𝑡𝑖𝑡𝑢𝑡𝑒 3 − 6%

चलो चलें िवाई लेने एंटी CONVULSION का

𝑺𝒕𝒂𝒈𝒆 − 𝟎𝟐

𝑼𝒏𝒆𝒒𝒖𝒊𝒗𝒐𝒄𝒂𝒍 𝑺𝒍𝒆𝒆𝒑 𝐶𝑜𝑛𝑠𝑡𝑖𝑡𝑢𝑡𝑒 40 − 50%

Cl-

𝑺𝒕𝒂𝒈𝒆 − 𝟎𝟑

α

𝑫𝒆𝒆𝒑 𝒔𝒍𝒆𝒆𝒑 𝒕𝒓𝒂𝒏𝒔𝒊𝒕𝒊𝒐𝒏

GABA Site

β α

𝐶𝑜𝑛𝑠𝑡𝑖𝑡𝑢𝑡𝑒 5 − 8%

Chloride Channel Wide open

𝑺𝒕𝒂𝒈𝒆 − 𝟎𝟒

𝑪𝒆𝒓𝒆𝒃𝒓𝒂𝒍 𝑺𝒍𝒆𝒆𝒑

𝐶𝑜𝑛𝑠𝑡𝑖𝑡𝑢𝑡𝑒 10 − 20% Cell

Membrane

Different stages of Sleep pattern

Sedation − Sleep − Anaesthasia − Coma

𝐋𝐨𝐧𝐠 𝐀𝐜𝐭𝐢𝐧𝐠

Hypnotics are the drugs which make person calm but also induce sleep. This is extension of sedative dose of any drugs. Sedative in large dose act as hypnotics E Mail- [email protected] Reach solution at- www.facebook.com/pharmavideo/

𝐁𝐚𝐫𝐛𝐢𝐭𝐮𝐫𝐚𝐭𝐞

Phenobarbitone

HYPNOTICS

𝑹𝑬𝑴 𝒔𝒍𝒆𝒆𝒑

GABA Site

𝑷𝒂𝒓𝒂𝒅𝒐𝒙𝒊𝒄𝒂𝒍 𝑺𝒍𝒆𝒆𝒑 β α

α

𝐶𝑜𝑛𝑠𝑡𝑖𝑡𝑢𝑡𝑒 20 − 30%

BZD Site

γ

α

Benzodiazepine Mechanism Schematic Diagram

Mechanism of Action Target of Benzodiazepine are on GABA receptor, because GABA is major inhibitory neurotransmitter in CNS. GABA is consisting of five- alpha, beta, gamma subunits that span the postsynaptic membrane. The influx of chloride Ions cause hyper polarization of the neuron and decrease neurotransmitter by inhibiting the formation of action potentials. Empty receptor is inactive and coupled chloride channel is closed www.facebook.com/pharmavideo/

Binding of GABA open the chloride channel cause hyper polarization

Pharmacological Action

Reduction of Anxiety Sedative-Hypnotics Anterograde Amnesia Muscle Relaxant

Mechanism of Action in various steps Entries of chloride hyper polarize cells, make them difficult to depolarize and reduce neural excitability

Binding of GABA is enhanced by benzodiazepine; result in more entry of negative chloride ions.

By Targeting GABA receptor

E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

Methods Available for Sterilization

Mostly Preferred over Chemical

PHYSICAL

Sunligh t

Heat

CHEMICAL

Filtration

Radiation Non-Ionizing & Ionizing Radiations Electromagnetic- Particulate

GAS

Liquid s

Below 1000C

Dry Heat

At 1000C

Moist Heat

Ethylene Oxide Formaldehyde

Above 1000C

Autoclave Hot Air Oven, Red Heat, Infrared, Flaming, Incineration

Alcohol Aldehydes Phenolics Halogens Heavy Metals Surfactants Dyes

Earthen ware, Asbestos, Sintered glass, Membrane Good for Large Surface Area Pressure Vent

Pressure Meter

Steam Circulation

Object to be sterilized

Water Vapor

Inner Stand

1. Liquid media 2. Nonflammable liquids 3. Glassware: empty and inverted 4. Dry hard items, either unwrapped or in porous wrap 5. Metal items with porous parts 6. Pipette tip boxes www.facebook.com/pharmavideo/

Outer Jacket

Heating Coil

Autoclave Stands

PRINCIPLE (Autoclave) www.facebook.com/pharmavideo/

Water inside autoclave converts into vapor and create pressure and when object containing M.O. is placed inside the autoclave this moist heat + Vapor coagulate the protein of Microorganism and finally killed them. It is more powerful than dry heat. ©Solution-Pharmacy- Freely uses this image but please give Solution URL as your reference. (PP)

E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

PUSHPENDRA KUMAR PATEL*

Short Description on

Organ Bath Assemblies https://www.facebook.com/pharmavideo/

Figure- solution/SOB*- Labelled diagram of student organ bath

Introduction- Student organ bath or simply organ bath is an apparatus widely used in pharmacology laboratory and various educational Institutes, research and development sector. Organ bath is not a single apparatus but it is a combination of many small units which include1. Bath chamber 2. Organ tube 3. Glass coil 4. PSS reservoir 5. Heater 6. Thermostat 7. Stirrer or mixer 8. Oxygen tube 9. Aerator 10. Leaver 11. Load 12. Sherrington rotating drum (Kymograph Drum) 13. Kymograph Paper Use- When we have to perform the invitro studies of any given drug, we need to isolate the organ from suitable experimental animal. Once organ is isolated it should be immediately transferred into physiological salt solution (PSS). Organ bath is having several important component and assembly as mentioned above; all are equally important and have individualized functions. Once organ is placed into PSS other arrangement are made. These includePage | 1 https://www.facebook.com/pharmavideo/ *This notes and diagram is made by solution pharmacy, exclusively for pharmacy students

1. 2. 3. 4.

Cleaning the organ bath assembly Attaching or arranging all small hooks, clamp and water pipes. Fixing the lever and stick the kymograph paper on rotating drum. Kymograph paper should be either smoked or have to use colour ink at the end of lever. 5. Fill the water into 2/3 portion of organ bath or up to suitable length depending upon the unit of organ bath. 6. Switch on the mains and heater 7. Wash the organ tube with PSS once 8. Fill the PSS into organ bath and hold it. 9. Start providing oxygen by aerator machine 10. Attach the aeration tube into the organ bath 11. Now tie the tissue of isolated organ which you have to study (This process may be modified) 12. Tie the other end of thread into writing lever 13. Attach the lever with rotating drum and wait till resting or constant line appears 14. Inject the drug into organ bath and carefully examine the changes in muscle strength by observing kymograph paper. 15. Release the clamp of organ bath to let the PSS flow outside the organ tube if you want to reduce the strength of dose, if you want to increase the dose, no need to change the PSS. (It is for same drug) 16. For every new drug injection the old PSS must be change. 17. Ensure the temperature of water bath; it should not increase than optimum temperature.

Description of various parts

1. Bath chamber- Bath chamber is made of good quality plastic (PVC) it is of two typesSingle unit and double unit. In single unit there is only one place for organ tube, thus you can perform one study at one time, or you need to wash the tissue with PSS before changing drug. Double unit organ bath is having two holding place for organ tube, that’s why we can perform two studies at same time. It depend on you weather you want to check the effect of various dose of same drug or you can check two separate drug’s effect on muscle. At the bottom of bath chamber there is two outlets, one is for drainage of water and second is for the PSS. 2. Organ Tube- Organ tube is the soul of organ bath because the king of experiment lies or rest in this chamber. Organ tube is a glass tube having two sides opening. Out of which one is for expelling used PSS and second is for inlet of PSS. PSS is not filled directly from the top of organ tube, but it is filled from this side inlet unit. Page | 2 https://www.facebook.com/pharmavideo/ *This notes and diagram is made by solution pharmacy, exclusively for pharmacy students

3. Glass coil- Glass coil is coil like structure (As name indicate) its function is very simple. If we supply PSS directly to the organ tube from straight pipe, its temperature may not be equal to outer temperature that is about 370C, so the PSS is supplied through this pipe, by doing so the PSS take a longer time to reach organ tube and contact time of PSS increase with water available in the bath chamber and this the temperature of PSS slightly increase and matched with outer temperature. 4. PSS reservoir- PSS reservoir is a simple vessel which holds PSS to be supplied to organ in organ tube. PSS is essential solution containing all electrolytes which are necessary for the intact tissue. These include maintenance of is tonicity, conductivity and contractility etc. Example of PSS includes- (1) Frog ringer solution (2) Ringer or Ringer Locke solution (3) De Jalon solution (4) Tyroid solution (5) Kerbs-Henslet solution. 5. Heater-

Heater is heating devices which maintain the desired (370C) temperature of water inside the organ bath. Optimum temperature is important for the tissue attached in a organ bath, because this help to maintain its live condition. And the contraction or relaxation of muscle may affected by variation in temperature.

6. Thermostat-

Thermostat is very basic devise available in every home. The objective of Thermostat is to maintain the temperature we have set. Thermostat is based on auto cut principle. When the temperature exceed from set temperature, it automatically stop the heater, and once when temperature start falling it again start the heater so that water start heating.

7. Stirrer or Mixer- Stirrer is a device or part of devise which is used to homogenize the temperature of water inside the organ bath. If we don’t use stirrer the temperature of water may vary part to part and this is not suitable for tissue. So the basic work of mixer is to mix the heat throughout the water bath. 8. Oxygen Tube- Oxygen tube is one of the most important parts of student organ bath. Oxygen tube carries oxygen directly to the tissue tied. Tissue is tied at the end of oxygen tube and it gets oxygen form this tube which is fitted to aerator at the other end. One end of aerator tube is consisting of thin metal wire and in this metal wire we tied the tissue and the other end of tissue will be tied with the lever. Any changes in the tissue will be recorded in the kymograph paper by the lever. 9. Aerator-

This is a common device used to supply the vital air that is oxygen. It generates oxygen and pump to the aeration tube where our tissue is located. Aerator is also used in the aquarium and the purpose is same, to generate and supply oxygen to the tissue.

Page | 3 https://www.facebook.com/pharmavideo/ *This notes and diagram is made by solution pharmacy, exclusively for pharmacy students

10. Lever-

This is the main part of any organ bath. Lever is a simple writing device which records every movement or changes in the strength of muscle by drug we applied. One end of the lever is attached to the tissue and when we inject the drug into the organ tube, its effect can be easily seen in muscle, either in form of contraction or relaxation. When muscle get contracted it pull the thread and thread pulls the lever and it may seen by upward graph and the opposite is applicable for muscle relaxation. There are various types of lever available- (1) Simple lever (2) Frontal lever (3) Starling’s heart lever (4) Brodie’s Universal lever (1) Diagram of Frontal Lever

(2) Frontal Lever

(3) Diagram of Starling’s heart lever

11. Load-

Load is nothing but an object which provide optimum load and tension to the lever so that proper recording will be achieved.

12. Sherrington rotating drum (Kymograph Drum) - It is another main parts or assembly of student organ bath. It is a rotating devise, which keep rotating and recording the changes in tension of lever. It has several basic units’ like- gear and clutch which allow us to set the desired RPM (rotation per minutes) at the back of this there is a lock which lock and unlock the machine. In front of the devise there is counter which count the RPM by touching the other hand. Kymograph is attached with kymograph paper, this is used either by coating with smoke or by using colour pen.

References- All materials and notes are made by solution pharmacy

Page | 4 https://www.facebook.com/pharmavideo/ *This notes and diagram is made by solution pharmacy, exclusively for pharmacy students