Renal Pharmacology Flashcards
osmotic diuretics MOA
The proximal tubule and descending limb of Henle’s loop are freely permeable to water.
An osmotic agent that is not reabsorbed causes water to be retained in these segments and promotes a water diuresis.
They also oppose the action of ADH in the collecting tubule.
The prototypic osmotic diuretic is ?
mannitol
pk of osmotic diuretics
Osmotic diuretics are poorly absorbed, which means that they must be given parenterally.
If administered orally, mannitol causes osmotic diarrhea. Mannitol is not metabolized and is excreted primarily by glomerular filtration within 30–60 minutes,
Indication for osmotic diuretics / therapeutic use
treatment for patients with increased intracranial pressure or acute renal failure due to shock, drug toxicities, and trauma
ADRs of osmotic diuretics
Extracellular Volume Expansion
Dehydration and Hypernatremia
Vasopressin (Antidiuretic Hormone, ADH)
Vasopressin is a peptide hormone released by the posterior pituitary in response to rising plasma tonicity or falling blood pressure.
deficiency of ADH results in
diabetes insipidus
PK of ADH
Vasopressin is administered by intravenous, intramuscular, or intranasal routes; oral absorption is slight.
The half-life of circulating ADH is approximately 20 minutes, with renal and hepatic metabolism.
A small amount of vasopressin is excreted as such in the urine.
MOA of ADH
Vasopressin interacts with two types of receptors.
V1 receptors are found on vascular smooth muscle cells and mediate vasoconstriction
V2 receptors are found on renal tubule cells and mediate antidiuresis through increased water permeability and water resorption in the collecting tubules.
The long-acting synthetic analog of vasopressin is?
Desmopressin acetate (DDAVP) with minimal V1 activity and an antidiuretic-to-pressor ratio 4000 times that of vasopressin.
Clinical Pharmacology / Therapeutic use
Vasopressin and desmopressin are the alternative treatments of choice for pituitary diabetes insipidus.
Bedtime desmopressin therapy treats nocturnal enuresis by decreasing nocturnal urine production.
Vasopressin infusion is effective in some cases of esophageal variceal bleeding and colonic diverticular bleeding.
Toxicity & Contraindications of ADH
Headache, nausea, abdominal cramps, agitation, and allergic reactions occur rarely. Therapy can result in hyponatremic convulsions.
Vasopressin (but not desmopressin) can cause vasoconstriction and should be used cautiously in patients with coronary artery disease.
Nasal inhalation of desmopressin may be less effective when nasal congestion is present