P1 - PHARMACODYNAMICS

CARMUSTINE

A. Non – target protein mediated mechanism

Counterfeit incorporation mechanism

• anti cancer

• Alkylating agent

Target protein

--- biologic site of action of drugs

Structural protein

• collagen

• keratin

constitute “ cytoskeleton”

• Most abundant class of protein

• EX?

Microtubule (tubulin)

• important site of action

• Drugs that inhibit microtubule synthesis/ spindle protein

Podophyllum peltatum

Etoposide

• source

Regulatory Proteins

• mediates the transmission of endogenous chemical signals such as neurotransmitters, autacoids, and hormones

Channels/transport

› Proteins that take part in transmembrane signaling and regulates ionic composition

Voltage-gated Na channel

allow entrance of: Na

Voltage-gated Ca channel

allow entrance of: Ca

• Local anesthetics,

• Car Bama Zepine

• Phenytoin

Na channel blockers

• DRUGS

• L-type blockers (“-dipine”)

• T-type blocker - ethosuximide

Ca++ channel blocker

• types

L

____ -type blockers - NIFEdipine

T

_____ -type blocker - ethosuximide

Digoxin (increase heath act)

• heart

• potassium

• sodium

Na+-K+ ATPase pump

• INHIBITOR

  • Locate

  • pumasok

  • lumabas

Proton Pump Inhibitor (Peptic Ulcer)

• Stomach

• Potassium

• Proton

H+-K+ ATPase pump

• INHIBITOR

  • Locate

  • pumasok

  • lumabas

Furosemide (diuretic)

Na+-K+-2Cl- cotransport

• INHIBITOR

  • Locate

  • pumasok

  • lumabas

allopurinol

Xanthine oxidase

• INHIBITOR

NSAID's

Cyclooxygenase

• INHIBITOR

LIPOoxygenase

ARACHIdonic ACID

• product cause

gastric irritation

NSAID's

• ADR

Prostaglandin 1

produce: Cytoprotective

Prostaglandin 2

objective inflammation

• Mas potent inflam effect

ACE inhibitors

ACE (Angiotensin-converting enzyme)

• INHIBITOR

JUXTA glomerular CELL

Renin

• from

DRY cough

ACE inhibitors

• ADR

BRADYkitin

if we give ACE inhibitors no one will metabolized to

ΜΑΟΙ

MAO(monoamine oxidase)

• INHIBITOR

• Dopamine

• NorEpinephrine

• Epinephrine

MAO (monoamine oxidase)

• Responsible to metabolize

• Phenelzine

• Isocarbozaxid

• TranylCypromine

MAO (monoamine oxidase)

• DRUGS

Edrophonium

Acetyl Cholines Terase

• INHIBITOR

• Entacapone,

• Tolcapone

Catechol

O

Methyl

Transferase

• INHIBITOR

Dopamine

Important in EXTRApyrimidal system

• for movement