1 - pharmacodynamics

b. Type II receptors

b. Type II receptors

1. The largest family of receptors

   a. Type I receptors

   b. Type II receptors

   c. Type III receptors

   d. Type IV receptors

B. NR

ratio: Estrogen is a type of sex hormone

2. Estrogen binds to what receptor type

   A. LGIC

   B. NR

   C. GPCR

   D. ELR

c. Gq

3. Phospholipase C is activated by

   a. Gi

   b. Gs

   c. Gq

   d. AOTA

b. pharmacodynamics

4. what the drugs does to the body?

   a. pharmacokinetics

   b. pharmacodynamics

   c. Pharmaceutics

   d. Pharmacovigilance

a. Insulin (for IDDM)

5. Which of the ff is a replenisher

   a. Insulin (for IDDM)

   b Paracetamol (for HA)

   c. Azithromycin (for bacterial tonsilitis)

   d. Cyclophosphamide (for breast CA)

a. Type 1

6. Ionotropic Receptors

   a. Type 1

   b. Type 2

   c. Type 3

   d. Type 4

d. Type 4

7. Sex hormones belong to what type of receptor?

   a. Type 1

   b. Type 2

   c. Type 3

   d. Type 4

d. Edrophonium

8. Which of the ff is a diagnostic agent?

   a. Buspirone

   b. Diazepam

   c. Telithromycin

   d. Edrophonium

b. cAMP level

9. Activation of Gs leads to the activation of

   a. ion flux

   b. cAMP level

   c. TKA

   d. lipophilic nature of drug

a. Levodopa for Parkinsonism

10. which of the ff is an example of replenisher

    a. Levodopa for Parkinsonism

    b. Isoniazid for Tuberculosis

    c. Paracetamol for HA

    D. Cyclophosphamide for breast cancer

Drug Effect

this deals w/ biochemical and physiological effects of Drug.

Drug Action

this deals w/ mechanisms involved by which they produce such effects

Functional Modifiers

• MOST COMMON type of drugs

• alter the normal physiology or processes in the human body

Replenishers

supplement the existing endogenous compound that are deficient or lacking in concentration

• Alteration of Anxiety - (Diazepam, Buspirone; chronic anxiety dis)

• Alteration of Pain - Morphine;Narcotic analgesic, Paracetamol; Fever;Pain

examples of Functional Modifiers

• IDDM - Type 1 DM  (Insulin: Glargine, Aspart)

• Diarrhea - OR

• Folate Deficiency (can lead to megaloblastic anemic) - Folic Acid Vitamin B9

Examples of Replenishers

Diagnostics

used to determine the presence/absence of diseases

• Tensilon test (Edrophonium): presence of Myasthenia Gravis

• Barium Sulfate (barium meal) - GIT disorders

• Mechacholine - For Broncho provocation Test (diagnosis for asthma)

examples of Diagnostics

Chemotherapeutics

• Kill or inhibit the growth of cancer cells (anti-neoplastics)

• Kill or inhibit the growth of microbes (anti-microbials)

• Alkylating agents (Cyclophosphamide); for breast cancer

• Doxorubicin

examples of chemotherapeutic drugs that kill or inhibit the growth of cancer cells (anti-neoplastics

• Antibacterials;penicillin, cephalosporins

• Anti-virals

• Anti-fungals

examples of chemotherapeutic drugs that kill or inhibit the growth of microbes (anti-microbials)

Receptors

• protein molecules (receptor) which bind a chemical signaling molecule (ligand)

• undergoes a conformational change which activates signaling pathway to bring a cellular response

Type 1

What type of Receptor?

Ionotropic or Ligand-gated ion channel Receptors

Type 2

What type of Receptor?

G-protein-coupled receptors (Metaboprotic)

Type 3

What type of Receptor?

Enzyme-linked receptors (Tyrosine-Kinase Receptor)

Type 4

What type of Receptor?

Nuclear receptors

Ligand-Gated Ion Channels

• Aka Inotropic Receptor

• Extracellular portion of usually contains the ligand-binding site

• Channel is usually closed until the receptor is activated by an agonist, which opens the channel briefly for a few milliseconds

Type 1

The ff is belong to what what type of receptor?

GABA receptor increases chloride influx → Hyperpolarization

Type 1

The ff is belong to what what type of receptor?

Nicotinic receptor increases Sodium influx → Depolarization

G protein-coupled receptor

• Aka 7-TM receptors (because they have 7 transmembrane domains), or Metaboprotic

• Extracellular domains determine ligand binding and selectivity

• Intracellular loops mediate the receptor interaction with its EFFECTOR MOLECULE, a guanine nucleotide binding protein (G protein), a peripheral membrane protein

cAMP

Adenyl Cyclase stimulates what type of second messenger?

DAG & IP3

Phospholipase C stimulates what type of second messenger?

Gas or Gs

Adenyl Cyclase is activated with by what type of G-protein coupled receptor?

Gai or Gi

Adenyl Cyclase is inhibited by with what type of G-protein coupled receptor?

Gaq or Gq

Phospholipase C is activated by with what type of G-protein coupled receptor?

Increase of cAMP

Activating Gas/Gs leads to an ___ of cAMP

decrease of cAMP

Inhibiting Gai/Gi leads to a ___ of cAMP

increase DAG, IP3

stimulating Gaq/Gq leads to an ___ of DAG, IP3

IP3

a second messenger that regulates intracellular calcium, as well as some protein kinases

Alpha 1

Gq is coupled with what type of adrenergic receptor?

Alpha 2

Gi is coupled with what type of adrenergic receptor?

Beta 1 & Beta 2

Gs is coupled with what type of adrenergic receptor?

vasoconstriction

Activation of alpha 1 can cause:

decrease Norepinephrine release

Activation of alpha 2 can cause:

Increase Heart Rate

Activation of beta 1 can cause:

bronchodilation

Activation of beta 2 can cause:

Enzyme-linked receptor

Aka tyrosine kinase receptor

• Drug binding

• Dimerization - Dimer formation

• Phosphorylation

Processes of Enzyme-linked receptor

Phosphorylation

This can substantially modify the structure of the target protein, thereby acting as a molecular switch.

• Insulin Receptor + Activation of Tyrosine Kinase = increase Glucose uptake

• Atrial Natriuretic Factor Receptor  = stimulates Guanyl Cyclase = increase Na sectretion

examples of Enzyme-linked receptor

Nuclear Receptor

• Entirely intracellular

• Drug must be lipophilic

• Drug interacts to the DNA → gene transcription

NR Type 1: Steroid Receptor

• Steroid is lipophilic, so it can enter the cell membrane 

• Steroid will bind to steroid receptor

• hsp will be dissociated

• dimerization of steroid receptor

• Steroid enters the nucleus = affects the DNA synthesis = GENE TRANSCRIPTION

NR Type 2: Non-steroid Receptor

• Ex. Vitamin A & D (they are lipophilic)

• NO binding with steroids = receptor is already present in nucleus = RESPONSE

Cell Membrane

Location of Ligand-Gated Ion Channels

Cell Membrane

Location of G protein-coupled receptor

Cell Membrane

Location of Enzyme-linked receptor

Nucleus

Location of Nuclear Receptor

Ion Flux

Main action of Ligand-Gated Ion Channels

cAMP, DAG, IP3

Main action of G protein-coupled receptor

Phosphorylation

Main action of Enzyme-linked receptor

Gene Transcription

Main action of Nuclear Receptor

Ligand-Gated Ion Channels

GABA-a Nicotinic receptor is an example of

G protein-coupled receptor

Adrenergic receptors is an example of

Enzyme-linked receptor

Insulin receptor is an example of

Nuclear Receptor

Steroid receptor (Sex hormones), and non-steroids are example of