ORG MED CHAP 1 Flashcards
It is the practice of medicinal chemistry that is devoted to the discovery and development of new drugs
Organic Medicinal Chemistry
an agent intended for use in the diagnosis, mitigation, treatment, cure, or prevention of disease in humans or in other animals
Drug
___________ is a substance to which a drug needs to interact with to elicit a pharmacological response
___________proteins, some are nucleic acids and lipids
receptor is a substance to which a drug needs to interact with to elicit a pharmacological response
90% proteins, some are nucleic acids and lipids
___________ ability of drug to bind to the receptor
Affinity
___________ ability of a drug to exert a pharmacologic action
INTRINSIC ACTIVITY ability of a drug to exert a pharmacologic action
_______
Affinity only
ANTAGONIST
_________
Affinity + Intrinsic activity
AGONIST
WHAT ARE THE FOUR FUNDAMENTAL PATHWAYS OF DRUG PHARMACOKINETICS?
(ADME) ABSORPTION, DISTRIBUTION, METABOLISM AND EXCRETION
_____________________
site other than the binding site
ALLOSTERIC SITE
_______________
the transfer of a drug from its site of administration to the systemic circulation (or
to the bloodstream)
ABSORPTION
WHAT ARE THE FACTORS THAT INFLUENCE THE
ABSORPTION?
Chemical structure
Variation in particle size
Nature of the crystal form (Amorphous >
Crystalline)
____________ = 100% crystalline (long-acting)
Ultra-lente
____________= 70% crystalline, 30% amorphous
(intermediate)
Lente insulin
_________ = 100% amorphous (short-acting)
Semi lente
What is the minimum value of Pre- Diabetes?
100
what is the maximum value of Diabetes?
above 126
what is the maximum value of Pre-Diabetes?
125
what is the minimum value of Diabetes?
126
it is the fraction of administered drug that reaches the systemic circulation in a chemically
unchanged form (f)
Bioavailability
it is the process by which a drug reversibly leaves the bloodstream and enters the interstitium (extracellular fluid) and/or the cells of the tissues
DISTRIBUTION
________________
- serves as a reservoir
-may limit access to certain body
compartments
- Prolongs drug duration of action
PLASMA PROTEIN BINDING
___________binds acidic drugs
Albumin
__________binds basic drugs
α-1-acid-glycoprotein
___________________
* converts drugs into polar form, water-soluble products that are readily excretable
* detoxification process but not all the time
METABOLISM
compounds that are inactive in their native form, but are easily metabolized to the active agent
Ex:
– Enalapril to Enalaprilat
– Chloramphenicol palmitate to Chloramphenicol
– Primidone to Phenobarbital
– Phenacetin to Paracetamol
PRODRUGS
GIVE ME ONE EXAMPLE OF FIRST PASS EFFECT
NITROGLYCERIN
______________
* drugs may be metabolized by hepatic enzymes to inactive chemicals (drug is metabolized prior to absorption)
* only _________ administered orally and
rectally undergo first pass metabolism (CYP 450)
FIRST PASS EFFECT
DRUGS
__________________
* the main route of excretion of a drug and its metabolite is through the kidney (for LMW & polar drugs)
EXCRETION
WHAT ARE THE OTHER TYPES OF EXCRETION?
Biliary/Fecal, Breastmilk, Sweat (for HMW & lipophilic drugs)
A drugs emptied via the bile duct into the small intestine can be reabsorbed in the intestinal lumen back to systemic circulation
ENTEROHEPATIC RECIRCULATION
