PMOC M1 Flashcards
INTRODUCTION M1
According to Drugbank how many drugs available worldwide.
16579
who make those drugs
Scientist and Chemist
MEDICINAL CHEMISTRY
An interdisciplinary science
- Organic Chemistry
- Biochemistry
- Computational Chemistry
- Pharmacology
- Pharmacognosy
- Molecular biology
- Physical Chemistry
The primary objective of medicinal chemistry is the design and discovery of new compounds that are suitable for use as drugs.
MEDICINAL CHEMISTRY
Branch of chemistry involved in identification, design, synthesis, and development of biologically active compounds.
MEDICINAL CHEMISTRY
Goal: Design a drug that will interact as powerfully and selectively as possible for the target
Pharmacodynamics
are low MW chemical substances that interact with macromolecular targets in the body to produce effect
DRUGS
SAR
Structure activity relationship
to define the relationship between the chemical compound and the pharmacological activity mechanism of action in site in the body
Structure Activity Relationship
Foreign substances = stranger = called ———-
XENOBIOTICS
Goal: Design the drug so that it is capable of reaching that target
Pharmacokinetics
When the conventional dosage forms are administered orally or topically, the active drug in the dosage form is immediately released and absorbed into the systemic circulation.
Liberation
higher concentration to lower concentration for your drug to diffuse in to your system
Diffusion
unbound drug is passively filtered by the glomerulus.
Glomerular Filtration
majority of the drug is actively secreted
Tubular Secretion
NONIONIZED OR UNIONIZED = drug is passively reabsorbed back into the blood.
Tubular Reabsorption
Excretion into the urine is a major route of elimination for metabolites and unchanged drug.
DRUG EXCRETION
- Drug reenters the intestinal tract from the liver through bile duct
- Biliary recycling
ENTEROHEPATIC CIRCULATION
- Decreased metabolism
ENZYME INHIBITION
- Increased metabolism
ENZYME INDUCTION
– antiarrhythmic [60% is metabolized when given orally]
LIDOCAINE
- A significant proportion of a drug is metabolized by hepatic enzyme during the initial trip through the liver
- Drug removal by the liver after absorption
- happen in metabolism
FIRST-PASS EFFECT
- All substances in the circulatory system, including drugs, metabolites, and nutrients, will pass through the liver.
- Most molecules absorbed from the GIT enter portal vein and are initially transported to the liver.
DRUG METABOLISM [BIOTRANSFORMATION]
- Delivery of drug to the tissue is controlled by the specific blood flow to a given tissue
Perfusion
- Drug movement from the systemic circulation going to different organs and tissues
- Blood Flow
DRUG DISTRIBUTION
- Protects the brain from exposure to chemical and metabolites, due to the presence of tightly joined epithelial cells lining the cerebral capillaries
Blood Brain Barrier
- Direct to Systemic Circulation
- Rapidly distributed
- IV, IM, SC, Intraspinal, Intracerebral
Parenteral Administration
- The most common and poplar route
ORAL ADMINISTRATION
Higher acidity [ph1.5-2 fed state;pH2-6 fasting state]
Full stomach
main site of absorption
- SMALL INTESTINE
Acidic Drug are more absorbed [ A + A ]
UNIONIZED
- Basic drug + Basic Medium
UNIONIZED
Acidic Drugs are more excreted [ A + B ]
IONIZED
- Acidic drug + Basic Medium
IONIZED
Bile describe
help the digestion and absorption of the fats
because of the active enzyme that release ng acid
secrete gastric acid
Higher Acidity in the full stomach 1.5-2pH level
organs that has high blood flow and perfusion rate
lung, kidney, and liver
Inactive form of drug to change in active form with the help of enzyme
Prodrug
what enzyme is prone in toxicity
Enzyme inhibitors
drug reenter
enterohepatic Circulation
3 effects in pharmacodynamics
- Therapeutic effect
- Subtherapeutic effect
- Toxic effect
doses/ concentration / target site correct
Therapeutic effect
decrease effectiveness
Subtherapeutic effect
doses/ concentration / target site not correct
Toxic effect
Distribution no need for absorption
Parenteral
Sublingual
is the most common mechanism controlling drug release.
diffusion
it is the biomolecules [protein/ nucleic acid]
Targets
carries active drug/ non-ionized drug
Blood Flow
it transforms active drug[unionized] into inactive[ionized] form to be eliminated ‘mostly’ but if not inactive form [ionized] turn into active will undergo Bioactivation
DRUG METABOLISM
also know as [BIOTRANSFORMATION]
Elimination has 2 process
- Metabolism
- Excretion
