This document discusses the mechanisms of drug action. It begins by explaining that drugs can produce effects through various mechanisms like interacting with enzymes, cell membranes, or other cellular components. It then describes four levels of drug action - molecular, cellular, tissue, and system. The document goes on to explain different types of effects like local vs systemic, primary vs side effects. It provides details on various mechanisms of drug action including physical mechanisms, chemical mechanisms, drug-receptor interactions, drug-enzyme interactions, drug-channel interactions, and miscellaneous mechanisms.
Histamine is a biogenic amine present in many animal and plant tissues that function as neurotransmitters and are also found in non-neural tissues, have complex physiologic and pathologic effects through multiple receptor subtypes, and are often released locally.
It is also present in venoms and stinging secretions. It is synthesized by decarboxylation of the amino acid, histidine. Histamine is mainly present in storage granules of mast cells in tissues like skin, lungs, liver, gastric mucosa, placenta, etc. It is one of the mediators involved in inflammatory and hypersensitivity reactions.
Histamine is a biogenic amine present in many animal and plant tissues that function as neurotransmitters and are also found in non-neural tissues, have complex physiologic and pathologic effects through multiple receptor subtypes, and are often released locally.
It is also present in venoms and stinging secretions. It is synthesized by decarboxylation of the amino acid, histidine. Histamine is mainly present in storage granules of mast cells in tissues like skin, lungs, liver, gastric mucosa, placenta, etc. It is one of the mediators involved in inflammatory and hypersensitivity reactions.
Pharmacodynamics is the study of the biochemical and physiological effects of drugs and their mechanisms of action. Pharmacodynamics is often referred to as “what the drug does to the body”.
In order to exert their effects, drugs usually interact in a structurally specific way with a protein receptor or act on physiological processes within the body. This activates a secondary messenger system that produces a physiological effect. Drugs do not create new action but they can only modify (alter) the functions of cells or tissues in body. The drug–receptor complex initiates alterations in biochemical and/or molecular activity of a cell by a process called signal transduction.
Pharmacokinetics - drug absorption, drug distribution, drug metabolism, drug ...http://neigrihms.gov.in/
A power point presentation on general aspects of Pharmacokinetics suitable for undergraduate medical students beginning to study Pharmacology. Also suitable for Post Graduate students of Pharmacology and Pharmaceutical Sciences.
This presentation contains drugs which blocks the adrenergic system e.g receptor blockers like alpha and beta receptor antagonists, adrenergic neuron blocking agents in details.various animated pictures are also included to make the presentation interesting as well as i have used various diagrams and tables to have better understanding of the topic. Thank you.
The slides describe concept of distribution, Volume of distribution, factors affecting volume of distribution and the barriers to distribution. Blood brain barrier and placental barrier.
An overview of muscarinic receptor agonists and antagonists. This presentation was delivered to 2nd year pharmacy students enrolled in a pharmacology & toxicology class and accompanies Goodman & Gilman's (12e) chapter 9.
Anti-inflammatory drugs
Inflammation is a normal, protective response to tissue injury caused by physical trauma, noxious chemicals, or microbiologic agents. Inflammation is the body's effort to inactivate or destroy invading organisms, remove irritants, and set the stage for tissue repair. When healing is complete, the inflammatory process usually subsides.
However, inflammation is sometimes inappropriately triggered by an innocuous agent, such as pollen, or by an autoimmune response, as in asthma or rheumatoid arthritis. Inflammation is triggered by the release of chemical mediators from injured tissues and migrating cells and include amines, such as histamine and 5-hydroxytryptamine; lipids, such as the prostaglandins; small peptides, such as bradykinin; and larger peptides, such as interleukin-l.
Pharmacodynamics is the study of the biochemical and physiological effects of drugs and their mechanisms of action. Pharmacodynamics is often referred to as “what the drug does to the body”.
In order to exert their effects, drugs usually interact in a structurally specific way with a protein receptor or act on physiological processes within the body. This activates a secondary messenger system that produces a physiological effect. Drugs do not create new action but they can only modify (alter) the functions of cells or tissues in body. The drug–receptor complex initiates alterations in biochemical and/or molecular activity of a cell by a process called signal transduction.
Pharmacokinetics - drug absorption, drug distribution, drug metabolism, drug ...http://neigrihms.gov.in/
A power point presentation on general aspects of Pharmacokinetics suitable for undergraduate medical students beginning to study Pharmacology. Also suitable for Post Graduate students of Pharmacology and Pharmaceutical Sciences.
This presentation contains drugs which blocks the adrenergic system e.g receptor blockers like alpha and beta receptor antagonists, adrenergic neuron blocking agents in details.various animated pictures are also included to make the presentation interesting as well as i have used various diagrams and tables to have better understanding of the topic. Thank you.
The slides describe concept of distribution, Volume of distribution, factors affecting volume of distribution and the barriers to distribution. Blood brain barrier and placental barrier.
An overview of muscarinic receptor agonists and antagonists. This presentation was delivered to 2nd year pharmacy students enrolled in a pharmacology & toxicology class and accompanies Goodman & Gilman's (12e) chapter 9.
Anti-inflammatory drugs
Inflammation is a normal, protective response to tissue injury caused by physical trauma, noxious chemicals, or microbiologic agents. Inflammation is the body's effort to inactivate or destroy invading organisms, remove irritants, and set the stage for tissue repair. When healing is complete, the inflammatory process usually subsides.
However, inflammation is sometimes inappropriately triggered by an innocuous agent, such as pollen, or by an autoimmune response, as in asthma or rheumatoid arthritis. Inflammation is triggered by the release of chemical mediators from injured tissues and migrating cells and include amines, such as histamine and 5-hydroxytryptamine; lipids, such as the prostaglandins; small peptides, such as bradykinin; and larger peptides, such as interleukin-l.
This presentation contains a detail account on how any drug acts and what are the receptors, its type etc. this may be helpful for quick understanding (digramatic).
A power point presentation on Pharmacodynamics (what drug does to the body) suitable for undergraduate medical students beginning to study Pharmacology
In pharmacology, the term mechanism of action (MOA) refers to the specific biochemical interaction through which a drug substance produces its pharmacological effect. A mechanism of action usually includes mention of the specific molecular targets to which the drug binds, such as an enzyme or receptor.
Principles and mechanisms of drug action. Receptor theories and classification of receptors, regulation of receptors. drug
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International Cancer Survivors Day is celebrated during June, placing the spotlight not only on cancer survivors, but also their caregivers.
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https://cansa.org.za/who-cares-for-cancer-patients-caregivers/
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2. Introduction
• A drug may produce its effects by a number of mechanisms
like combination with enzymes , cell membrane or other
components of a cell.
• The action either be physical or chemical and are classified at
four levels :
Molecular– Receptor, ion channel, enzyme, carrier molecules
Cellular– Transduction e.g., G protein, ion channel, enzyme
Tissue– Contraction, secretion, metabolic activity,
proliferation
System– CNS, CVS , etc.
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3. Types of effects
Local Effect
• When the drug effect occurs in immediate vicinity of
application, this is known as local effect.
Systemic Effect
• When the drug effect occurs away from the site of
administration, this is known as systemic effect.
Primary effect:
• Primary effect is the effect for which the drug is administered
or the treatment of the disease for which the drug is given.
Side effect:
• All other effects occurring in addition are known as secondary
effects. When the secondary effects are undesirable by the
patient, these are called adverse effects or side effects.9/21/2016 3
4. Mechanisms:
• Most drugs act by altering the various body control systems,
which may be receptors, enzymes or ion channels.
• These various mechanisms include:
1. Physical mechanisms
2. Chemical mechanisms
3. Drug- receptor interactions
4. Drug- enzyme interactions
5. Drug- channel interactions
6. Miscellaneous mechanisms
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5. Mechanism of Drug Action -
Physical Mechanisms
• When the drug does not produce any chemical
reaction or change in the cells of the body and the effect
is only physical, the mechanisms involved are called
physical mechanisms.
• These includes:
Local Application– Emollients, Counter irritants, Massagers,
pastes
Physically acting antacids– Milk, Mucin
Bulk forming purgatives– Bran, Ispaghula, Magnessium
sulphate
Mannitol
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7. Mechanism of Drug Action -
Chemical Mechanisms
• In chemical mechanisms, drugs act by producing chemical
reactions in the body.
• These include:
Chemically acting antacids– NaHCO3
Chelating agents– Dimercaprol, penicillamine,
desferrioxamine
Pralidoxime
9/21/2016 7
8. Mechanism of Drug Action -Drug
Receptor Interaction
• Receptor:
Macromolecules protein in nature which are target sites
for drugs.
Most drugs have to bind receptors to produce effects.
Receptors are located mostly on the cell membrane but
certain intracellular receptors are found as well.
9/21/2016 8
11. • The binding of drug with receptor may by of two types:
Reversible binding
Irreversible binding
• In reversible binding, the bond between the drug and
receptor is very weak ionic, hydrogen or van der wall. This the
effect is short lived.
• In irreversible binding, very strong covalent bonds are
present, which prolongs the effects of drug. The effect
continues until the drug is excreted or new receptor is
generated.
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12. There are three forms of binding to receptors:
• Agonists
• Antagonists
• Partial agonists
9/21/2016 12
14. Ligands
• Ligands are the endogenous substances, molecules or
compounds which bind with receptors present in the
body.
• e.g. acetyl choline, adrenaline, noradrenalin,
neurotransmitters like glutamate, aspartate and GABA.
• They produce various effects and interfere with the flow
of ions through channels called ligand gated channels.
• Their action may:
Resemble with natural ligand
Block the natural ligand
9/21/2016 14
15. Agonists
• They are the drugs which when bind receptors, cause
activation of receptors.
• They have the capacity to produce chain reactions in the
receptors which ultimately bring about the effects.
• Agonists have two properties:
Affinity for receptor
Capability to produce chain reactions in the cells having
capability of intrinsic activity or efficacy
9/21/2016 15
18. • When drug binds the receptor, activation occurs, and the
response gradually increases until it reaches the peak, then
the response decreases, although agonist still binds.
• This is due to desensitization of receptors, which might be
overcome by removing the agonists from the receptor.
• Example includes suxamethonium (succinyl choline), which
produces relaxation of skeletal muscles
9/21/2016 18
19. • Prolong contact of tissues with the agonists results in
decreased number of receptors in the tissues called down
regulation of receptors.
• Example includes the patients suffering from bronchial
asthma, in whom by prolong usage of beta agonists down
regulation occurs.
• This the effect is reduced.
9/21/2016 19
21. Antagonists:
• A substance which interferes with or inhibits the
physiological action of another.
• They have two properties:
Affinity
Do not have efficacy or intrinsic activity
• Examples include atropine, which is antagonist of acetyl
choline. Propanolol is antagonist of beta receptors.
9/21/2016 21
22. • The binding of antagonist with receptor is of two types:
Reversible binding
Irreversible binding
• Reversible binding is also known as competitive
antagonism. E.g. atropine.
• Irreversible antagonism occurs when binding effect of
antagonist is prolonged until drug is excreted or new
receptor is generated.
• Example includes phenoxy benzamine, which non-
competitively blocks action of catecholamines at beta
receptors.
• Second generation H1 histamines are also non-
competitive blockers.
9/21/2016 22
23. Partial antagonists
• They have intermediate levels of efficacy.
• They bind with the receptors but have very small
intrinsic activity and efficacy.
• Examples include beta blockers like pindolol and
oxpranolol.
9/21/2016 23
24. • Drugs having agonist effect at receptors have positive efficacy.
• Drugs having inverse agonist effect at receptors have negative
efficacy.
• Drugs having antagonist effect at receptors have zero efficacy.
Efficacy
9/21/2016 24
25. Mechanism of Drug Action -Drug
Enzyme Interactions
• Drug enzyme interaction is similar to drug receptor
interactions.
• The drugs resemble the natural substrates, bind enzymes and
cause change in their activity.
• This may take place by:
Activation of enzymes
Inhibition of enzymes
9/21/2016 25
26. • This combination of drugs with the enzyme may be:
Competitive
Non competitive
• Non competitive response is irreversible until new enzyme is
generated
9/21/2016 26
28. Non Competitive Inhibition
• The effects of non competitive inhibition are prolonged. These
include:
• Irreversible anticholinestrases e.g., Organophosphate
compounds
• Aspirin
• MAO Inhibitors e.g., Iproniazid, Phenelzine
• Proton Pump Inhibitors e.g., Omeprazole, Esomeprazole
9/21/2016 28
29. Mechanism of Drug Action -Drug
Channel Interactions
• In drug channel interaction, drug interfere with the flow
of ions through the channels specific for these ions.
• These include the Na+, K+,Ca++ and Cl- channels.
Examples include:
Sodium Channels:- Quindine Procainamide, Local
anesthetics
Calcium channels:- Nifedipine, Verapamil, Diltiazem
Potassium Channels:- Amiodarone, sulfonylureas
Chloride Channels:- Benzodiazepines
9/21/2016 29
30. Mechanism of Drug Action -
Miscellaneous Mechanisms
• Certain drugs do not act through any of the mechanisms
already mentioned, they are categorized as miscellaneous.
• These include:
Colchicines, vinca alkaloids
Ionizing radiation
Levamisole
Immunosuppressive:- Cyclosporine
Therapeutic antibodies
9/21/2016 30