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14 Cards in this Set

  • Front
  • Back

Excretion

Removal of drug and metabolites from the body. Kidney is most common, but also bile, lung and breast milk.

Renal excretion

Aka via the kidney. Majority of drug excretion. Limit duration and intensity of drugs. Decreased kidney function prolongs the duration of action and intensity of drug effects.

The nephron

Basic structural and functional unit if the kidney. Regulates water electrolyte and drug excretion, Ck trike blood volume,blood pressure, blood pH, and solute excretion.

Factors affecting renal drug excretion

Glomerular filtration, tubular secretion, tubular reabsorption.

Glomerular filtration

Drugs enter kidney from renal artery. Pressure within glomerulus forces low molecular weight drugs into the renal tubules. Lipid solubility and pH do not affect glomerular filtration of drugs. Only non protein bound drugs are filtered.

Tubular secretion

Drugs not filtered leave via efferent arteriole. Different arterioles divide to form capillaries that surround proximal tubules. Drugs can be secreted from blood into proximal tubule. Works one if two ways (for weak acids and one for weak bases).

Tubular reabsorption

Drugs move toward distal tubule their concentration increases due to loop of Henle. Once in distal tubule concentration exceeds that of it in the blood so uncharged lipophillic drugs just leave and go back into the blood.

Effect of age on renal function

Low for infants. By two it reaches normal amount. As we age it decreases.

Biliary drug excretion

Eliminated into bile then info the feces. For this they must 1) be molecular weight of >300 Da 2) have both polar and lipophillic groups (amphipathic) 3) are glucuronidated.

Bile excretion continued

Transporters on canalicular membrane if hepatocytes transport **** into bile. P-glycoprotein transports amphipathic drugs and MRP2 transports glucuronidated metabolites into bile. Either released in decreased or undergo enterohepatic recycling

Enterohepatic recycling

In the intestinal lumen. Bacteria cleave conjugated thing. Original drug reabsorbed. These drugs persist longer in the body.

Pulmonary drug excretion

Usually gasous and or highly volatile ex general anesthetics. Not heavily reliant on drug metabolism. Factors that effect it include 1) rate of respiration 2) cardiac output 3) solubility of drug in blood. High solubility=low excretion and vice versa.

Drug excretion in breast milk

>90% of woman take a drug first week. This means babies can be inadvertently exposed to drugs. These are 1)low protein binding 2) low molecular weight 3) high lipophilicity. Transporter breast cancer resistance protein BCRP puts it into the milk which las low pH and higher lipid content. Only few drugs do this though.

Other routes

Hair: we can see how long they've been exposed to it since it grows at 1cm per month. Saliva: drug is swallowed and either absorbed again or excreted in intestine. Sweat: washed away with minor amounts of reabsorption. These are minor compared to the first ones.