Singapore Drugs Database

Indication

For the treatment of Hypertension

Mechanism of Action

Possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, diltiazem, like verapamil, inhibits the influx of extracellular calcium across both the myocardial and vascular smooth muscle cell membranes. The resultant inhibition of the contractile processes of the myocardial smooth muscle cells leads to dilation of the coronary and systemic arteries and improved oxygen delivery to the myocardial tissue.

Pharmacokinetics

Absorption

Diltiazem is well absorbed from the gastrointestinal tract but undergoes substantial hepatic first-pass effect.

Distribution

Metabolism

Diltiazem is metabolized by and acts as an inhibitor of the CYP3A4 enzyme.

Elimination

Toxicity

LD₅₀=740mg/kg (orally in mice)

Active Ingredient/Synonyms

(+)-cis-5-[2-(dimethylamino)ethyl]-2,3-dihydro-3-hydroxy-2-(p-methoxyphenyl)-1,5-benzothiazepin-4(5H)-one acetate ester | (2S-cis)-3-(acetyloxy)-5-[2-(dimethylamino)ethyl]-2,3-dihydro-2-(4-methoxyphenyl)-1,5-benzothiazepin-4(5H)-one | (2S,3S)-5-(2-(dimethylamino)ethyl)-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]thiazepin-3-yl acetate | Acetic acid (2S,3S)-5-(2-dimethylamino-ethyl)-2-(4-methoxy-phenyl)-4-oxo-2,3,4,5-tetrahydro-benzo[b][1,4]thiazepin-3-yl ester | D-cis-diltiazem | Diltiazem | Diltiazemum | Diltiazem |

Indication

Magnesium chloride is used in several medical and topical (skin related) applications. Magnesium chloride usp, anhydrous uses as electrolyte replenisher, pharmaceutic necessity for hemodialysis and peritoneal dialysis fluids.

Mechanism of Action

Mechanism of action of magnesium chloride studied in 10 adult volunteers. Results suggested magnesium ion in duodenum is relatively weak stimulus to pancreas and gall bladder. It is weak stimulant to cholecystokinin release and inhibits net jejunal water absorption. The oral administration of a single 800 mg dose of magnesium chloride in healthy volunteers resulted in a diminished rate of intraluminal lipid and protein digestion. The most pronounced effect of magnesium chloride, however, was a decreased gastric emptying rate of both test meals. After correction for gastric emptying, no differences were noted in intraluminal lipid or protein digestion. Therefore, the lower lipid levels noted after magnesium supplementation are unlikely to be the result of altered lipid assimilation. Magnesium chloride slows gastric emptying but does not influence lipid digestion.

Pharmacokinetics

Absorption

Oral: Inversely proportional to amount ingested; 40% to 60% under controlled dietary conditions; 15% to 36% at higher doses

Distribution

Bone (50% to 60%); extracellular fluid (1% to 2%)

Metabolism

Magnesium levels are efficiently regulated by the kidneys. Magnesium also undergoes efficient enterohepatic circulation

Elimination

Clearance

Maximum magnesium clearance is directly proportional to creatinine clearance.

Toxicity

Mouse LD50 775mg/kg (intraperitoneal) Mouse LD50 : 7600mg/kg (oral) Rat LD 50 : 8100mg/kg (oral) Rat LD50 176mg/kg (intravenous) Severe toxicity occurs most often after intravenous infusions. It can also occur after chronic excessive oral doses, often in patients with renal insufficiency. Early manifestations are lethargy, hyporeflexia, followed by weakness, paralysis, hypotension, ECG changes (prolonged PR and QRS intervals), CNS depression, seizures, and respiratory depression. In overdose, magnesium impairs neuromuscular transmission, manifested as weakness and hyporeflexia.

Active Ingredient/Synonyms

Anhydrous magnesium chloride | Magnesium chloride anhydrous | Magnesium chloride |

Indication

For use as an electrolyte replenisher and in the treatment of hypokalemia.

Mechanism of Action

Supplemental potassium in the form of high potassium food or potassium chloride may be able to restore normal potassium levels.

Pharmacokinetics

Absorption

Potassium is a normal dietary constituent and under steady-state conditions the amount of potassium absorbed from the gastrointestinal tract is equal to the amount excreted in the urine.

Distribution

Metabolism

Elimination

Toxicity

The administration of oral potassium salts to persons with normal excretory mechanisms for potassium rarely causes serious hyperkalemia. However, if excretory mechanisms are impaired, of if potassium is administered too rapidly intravenously, potentially fatal hyperkalemia can result. It is important to recognize that hyperkalemia is usually asymptomatic and may be manifested only by an increased serum potassium concentration (6.5-8.0 mEq/L) and characteristic electrocardiographic changes (peaking of T-waves, loss of P-wave, depression of S-T segment, and prolongation of the QT interval). Late manifestations include muscle paralysis and cardiovascular collapse from cardiac arrest (9-12 mEq/L).

Active Ingredient/Synonyms

[KCl] | Chlorid draselny | Chloride of potash | Kaliumchlorid | KCl | Monopotassium chloride | Muriate of potash | Sylvite | Potassium Chloride |

Indication

This intravenous solution is indicated for use in adults and pediatric patients as a source of electrolytes and water for hydration. Also, designed for use as a diluent and delivery system for intermittent intravenous administration of compatible drug additives.

Mechanism of Action

Sodium and chloride — major electrolytes of the fluid compartment outside of cells (i.e., extracellular) — work together to control extracellular volume and blood pressure. Disturbances in sodium concentrations in the extracellular fluid are associated with disorders of water balance.

Pharmacokinetics

Absorption

Absorption of sodium in the small intestine plays an important role in the absorption of chloride, amino acids, glucose, and water. Chloride, in the form of hydrochloric acid (HCl), is also an important component of gastric juice, which aids the digestion and absorption of many nutrients.

Distribution

The volume of distribution is 0.64 L/kg.

Metabolism

The salt that is taken in to gastro intestinal tract remains for the most part unabsorbed as the liquid contents pass through the stomach and small bowel. On reaching the colon this salt, together with the water is taken in to the blood. As excesses are absorbed the kidney is constantly excreting sodium chloride, so that the chloride level in the blood and tissues remains fairly constant.Further more, if the chloride intake ceases, the kidney ceases to excrete chlorides. Body maintains an equilibrium retaining the 300gm of salt dissolved in the blood and fluid elements of the tissue dissociated into sodium ions and chloride ions.

Elimination

Toxicity

The rare inadvertent intravascular administration or rapid intravascular absorption of hypertonic sodium chloride can cause a shift of tissue fluids into the vascular bed, resulting in hypervolemia, electrolyte disturbances, circulatory failure, pulmonary embolism, or augmented hypertension. ( toxnet)

Active Ingredient/Synonyms

Sodium Chloride | Sodium Chloride |