DISTRIBUTION Flashcards
Total body fluid
42 liters
Intracellular
27 liters
Extracellular
15 liters
Intravascular
3 liters
Interstitial
12 liters
Properties of drugs that distribute intravascular:
Drugs with high molecular weight
Drugs are not filtered through the capillaries
Properties of drugs that distribute extracellular:
Drugs has small molecular weight
BUT can’t pass through the membrane (not lipid soluble)
Properties of drugs that distribute intracellular :
Drugs that have small molecular weight
Drugs that are lipid-soluble
Examples of drugs that distribute intravascular:
Heparin
Dextran
Plasma proteins
Drugs bound to plasma proteins
Examples of drugs that distribute extracellular:
Ions Quaternary ammonium (QA) compunds
Examples of drugs that distribute intracellular:
Tertiary amine (TA) compunds
Asprin
Ethanol
Tissue reservoir of iodine:
THYROID
Tissue reservoir of thiopentone
FAT
Tissue reservoir of Calcium ions:
BONES
Tissue reservoir of Digoxin:
HEART
Blood brain barrier formed of
Formed by brain capillary endothelium with tight junctions and adjacent glial cells
No water channels
Type of drugs that can pass throught blood-brain barrier
Only lipid-soluble, non-ionized drugs
Inflammation ……… permiability of drugs to the brain
increases
Area in the brain that doesn’t contain the blood brain barrier
Chemoreceptor trigger zone (CTZ) of medulla
Placental barrier is formed by:
Epithelium of fetal villi and capillary endothelium
Placental barrier is rich in ……..
Enzymes that inactivate drugs
Drugs that pass the placental barrier during pregnancy can be ….
teratogenic
Factors affecting distribution:
- Lipid solubility
- Molecular weight
- Ionization
- Binding to plasma proteins
- Difference of regional blood flow
- Precense of barriers
Highly-lipid soluble drugs get initially distributed to ……….. and ………. example
Organs with high lipid content ….. high blood flow ….. brain, heart and kidney
After the drug is distributed to high blood flow areas, it redistributes to ……. but ……. example ……
less vascular ….. more bulky tissues …… muscle and fat
Greater the lipid solubility of the drug, ………….. its redistribution
FASTER
In the plasma, the drug is present in 2 forms:
Free form
Bound form
The free form is: (4 characteristics)
- Active
- Filtered
- Metabolised
- Excreted
The bound form is: (4 characteristics)
- Not Active
- Not Filtered
- Not Metabolised
- Not Excreted —> has a prolonged action
What binds to acidic drugs
Albumin
What binds to basic drugs
alpha-1 acid glycoprotein
Plasma proteins have site for …… and ………. for drugs
competition …. displacement
Which drug displaces anti-coagulants?
Asprin
May lead to toxicity
Drugs that bind to the tissue-proteins of the heart:
Digitalis
Drugs that bind to the tissue-proteins of the thyroid :
Iodine
Drugs that bind to the tissue-proteins of the iris:
Ephedrine and atropine