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Octreotide-It is a long-acting octapeptide with pharmacologic properties mimicking those of the natural hormone somatostatin.

Octreotide is an octapeptide that mimics natural somatostatin pharmacologically, though it is a more potent inhibitor of growth hormone, glucagon, and insulin More

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Description

Octreotide is an octapeptide that mimics natural somatostatin pharmacologically, though it is a more potent inhibitor of growth hormone, glucagon, and insulin

Generic Name

Octreotide-It is a long-acting octapeptide with pharmacologic properties mimicking those of the natural hormone somatostatin.

Chemical names

Octreotide; Octreotidum [Latin]; Octreotide-LAR; Octreotide Acetate Salt, Octreotida [Spanish]

Brand names

Actide, Octate, Ferotide, Octide, Octreo,Octotide, Octride, Okeron, Octronis, Otide, Sandostatin Lar, Sandostatin

IUPAC name

(4R,7S,10S,13R,16S,19R)-19-[(2R)-2-amino-3-phenylpropanamido]-10-(4-aminobutyl)-16-benzyl-N-[(2R,3R)-1,3-dihydroxybutan-2-yl]-7-[(1R)-1-hydroxyethyl]-13-[(1H-indol-3-yl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17

Pharmacokinetics

Actions

Octreotide binds to somatostatin receptors. Octreotide binding to these receptors stimulates phosphotyrosine phosphatase and activation of the Na(+)/H(+) exchanger via pertussis toxin insensitive G proteins and coupled via pertussis toxin sensitive G proteins which lead to inhibition of adenylyl cyclase. 

Dosage/Dosage form

The recommended dose is 50-100 mcg twice a day as SC route, dose may increase up to 500 mcg. 

Therapeutic uses

For treatment of acromegaly and reduction of side effects from cancer chemotherapy

Adverse effects/Side effects

Local pain, stinging, tingling at site of inj; anorexia, nausea, vomiting, abdominal pain, bloating, flatulence, loose stools, steatorrhoea; biliary tract abnormalities. Hypoglycaemia and hyperglycaemia, hypothyroidism, cardiac conduction abnormalitles, pancreatitis.

Interaction

  • Dosage adjustment of concurrent therapy may be necessary with calcium channel blockers, oral hypoglycaemics, β-blockers, diuretics.
  • Requirements of insulin may be reduced requiring careful blood-glucose monitoring. Reduction in ciclosporin bioavailability and efficacy.
  • May increase concentration of bromocriptine.
  • Schedule injections between meals to decrease adverse GI effects.

Contraindications

Storage

Stable at room temperature for up to 14 days. Store at 2-8°C.

Information

Molecular weight

1019.25

Molecular formula

C49H66N10O10S2

CAS number

83150-76-9

Precautions

  • Monitor levels of vitamin B12 during long term therapy.
  • DM
  • Renal disease; risk of gall bladder disease.
  • Hypothyroidism
  • Pregnancy, lactation, children, elderly.