1.1 - Mechanisms of Action of Drugs Flashcards
Pharmacology
Study of drugs
Pharmacodynamics
Drug does to body
Pharmacokinetics
Body to drug
Pharmacotherapeutics
Rational use of drugs
Pharmacogenomics
Integrates differences in genetic of individuals
Classificattion based on General Use:
- Functional Modifier
- Replenishers
- Diagnostic Agents
- Chemotherapeutic Agents
Alters the physiologic and biochemical activity
Functional Modifier
– Beta blockers
– Antipyretics
Supplement endogenous substances that are insufficient
Replenishers
– Diabetes mellitus
– Peenicious anemia
Confirm/ Establish diagnosis of disease
Diagnostic Agents
– Tensilon Test
– Stress Testing
– Tc 99m Sestamibi and Thallium 20
Kill and inhibit growth of cells or multiplication of nucleic acids that are foreign to body
Chemotherapeutic Agents
– Anti infectives
– Antineoplastic
Target Protein Mediated Mechanism
- Structural Proteins
* Regulatory Proteins
Drugs that interfere with microtubules
- Colchicines
- Vinca
- Taxanes
- Estramustine
- Griseofulvin
Regulatory Proteins
- Voltage-gated ions — changes in membrane potential
- Carrier molecules — transport proteins; conformational changes
- Enzymes -
- Receptors
Carrier molecules
- Na-K ATPase Pump — (against concentration gradient) Digoxin
- K-H Pump/ PPI — PPI
Enzymes
- Phospholipase
- Cyclooxygenase
- 5-lipoxygenase
- MAO
Monoamine oxidase
- MAO-A — NE, EPI, 5-HT
* MAO-B — Dopamine
MAO Drugs (MPITS)
- Moclobemide
- Phenelzine
- Isocarboxazid
- Tranylcypromine
- Selegeline
Receptors
- Type I
- Type II
- Type III
- Type IV
Type I: Ionotropic/ Ligand -gated channel
- Nicotinic Receptor
- GABA-A Associated Ligand-gated
- Glycine Receptor
- 5-HT3 Receptor
Nicotinic Receptors – ACTIVATORS
- Nicotine
* Lobeline
Nicotinic Receptors – BLOCKERS
NMBs — Tubicurarine
GABAA Receptors – ACTIVATORS
- BZDs
- Barbiturates
- GABA
GABA A Recpetors – BLOCKERS
Flumazenil (BZD Binding Site)
Glycine Receptors – BLOCKERS
Strychnine
5-HT3 RECEPTORS – BLOCKERS
“-setron”
• Ondansetron
• Granisetron
• Palonosetron
Type II: Metabotropic/ 7-transmembrane Spanning/ G-protein coupled
- Gs
- Gi
- Gq
Gs — stimulates (⬆️ CAMP)
- Beta receptors
- 5-HT
- Histamine receptors
Gs ACTIVATORS
Catecholamine
Gs BLOCKER
Beta blockers (-“olol”)
Gi — inhibits (⬇️ CAMP)
- Presynaptic receptor a2
* PHT 1A receptor
Gi ACTIVATORS
Anti-HTNsives • Clonidine • Methyldopa • Guanfacine • Guanabenz
Gq — Contraction (stinulates PLC)
- a1 receptors
- Post synaptic a2 receptors
- M1 and M3 receptors
Gq ACTIVATORS
- EPI
- NE
- Dopamine
Gq BLOCKERS
- Prazosin
* Phenoxybenzamine
Type III: Tyrosine-Kinase Linked Receptor
- Insulin
- Gucokinase
- Glut II and Glut IV
- VEGFR
- TK Inhibitors
Type IV: Gene Transcription Link/ Nuclear Receptors
- Thyroid hormone
- Steroid hormone receptors
- Vitamin D and Vitamin D derivatives
Non Target Protein Mediated
– ✖️binding site
- Colligative/ Mass Effect
- Direct Chemical Interaction
- Counterfeit Mechanism aka Incorporation
Dependent on the # of solute particles in the soluton
— ⬇️ FP, ⬇️ VP, ⬆️ BP, OP
Colligative Mechanism
— Mannitol
Direct Chemical Interaction
- Neutralization
* Chelation
Neutralization
— Acid-base reaction
- Antacid for hyperacidity
- NAHCO3 for metabolic acidosis
- Protamine for Heparin Toxicity
Chelation
Deferoxamine for Iron (Fe) Poisoning
Counterfeit Mechanism aka Incorporation
Antimetabolites (Purine and Pyrimidine Analogs)
