1 / 20

Prepared by:

Somatostatin. Prepared by:. Mazen A. Basheikh. The Contents. Historical background. Actions & therapeutic uses. Side effects. Contraindication & precautions. Routes & Doses. Pharmacokinetics. What is it?. Historical Background.

marshall-green
Download Presentation

Prepared by:

An Image/Link below is provided (as is) to download presentation Download Policy: Content on the Website is provided to you AS IS for your information and personal use and may not be sold / licensed / shared on other websites without getting consent from its author. Content is provided to you AS IS for your information and personal use only. Download presentation by click this link. While downloading, if for some reason you are not able to download a presentation, the publisher may have deleted the file from their server. During download, if you can't get a presentation, the file might be deleted by the publisher.

E N D

Presentation Transcript

  1. Somatostatin Prepared by: Mazen A. Basheikh

  2. The Contents • Historical background. • Actions & therapeutic uses. • Side effects. • Contraindication & precautions. • Routes & Doses. • Pharmacokinetics.

  3. What is it?

  4. Historical Background • In early 1979, a chemist called Dr.Wilfried Bauer synthesized a compound with the research number SMS 201-995. The molecule was given the generic name octreotide, reflecting its structure with eight amino acids . • Subcutaneous Somatostatin was launched in 1988, and in 1991 it received the Prix Gallen. • The long-acting formulation, was launched in 1997. This provides patients with a more convenient treatment option via a single injection every 4 weeks.

  5. Where is it?

  6. Actions • Anterior pituitary GH TSH

  7. Gastrointestinal system • Somatostatin suppresses the release of gastrointestinal hormones: • Gastrin • Cholecystokinin (CCK) • Secretin • Motilin • Vasoactive intestinal peptide (VIP) • Gastric inhibitory polypeptide (GIP) • Lowers the rate of gastric emptying, and reduces smooth muscle contractions and blood flow within the intestine. • Suppresses the release of pancreatic hormones • Inhibits the release of insulin • Inhibits the release of glucagon • Suppresses the exocrine secretory action of pancreas.

  8. Therapeutic Uses • Acromegaly. • Tumors causing diarrhea like metastatic carcinoid & VIPomas. • Other causes of secretory diarrhea. • Decrease the GI secretions. • Insulinoma & correction of hypoglycemic drugs overdosage. • Varices associated with liver cirrhosis.

  9. Side Effects • >16%: • Endocrine & metabolic:Hyperglycemia . • Gastrointestinal: Diarrhea (36% to 58%), abdominal discomfort (5% to 61%), flatulence (<10% to 38%), constipation (9% to 21%), nausea (5% to 61%), cholelithiasis (27%; length of therapy dependent), biliary duct dilatation (12%),loose stools (5% to 61%), vomiting (4% to 21%)

  10. nervous system: Fatigue (1% to 20%), malaise (16% to 20%), dizziness (5% to 20%), headache (6% to 20%), fever (16% to 20%) • Cardiovascular: Sinus bradycardia (19% to 25%), chest pain (16% to 20%) • Hematologic:Antibodies to octreotide (up to 25%) • Local: Injection pain (2% to 50%; dose and formulation related) • Neuromuscular & skeletal: Backache (1% to 20%), arthropathy (16% to 20%) • Respiratory: Dyspnea (16% to 20%), upper respiratory infection (16% to 20%) • Miscellaneous: Flu symptoms (1% to 20%)

  11. 5% to 15%: • Endocrine & metabolic:Hypothyroidism (2% to 12%), goiter (2% to 8%) • Gastrointestinal: Abdominal pain, anorexia, cramping, dehydration, hemorrhoids, tenesmus (4% to 6%), dyspepsia (4% to 15%), steatorrhea (4% to 6%), feces discoloration (4% to 6%), weight loss • Cardiovascular: Conduction abnormalities (9% to 10%), arrhythmia (3% to 9%), hypertension, palpitation, peripheral edema • Central nervous system: Anxiety, confusion, depression, hypoesthesia, insomnia • Dermatologic: Pruritus, rash

  12. Genitourinary: UTI, renal calculus • Hematologic: Anemia • Hepatic: Hepatitis •  Neuromuscular & skeletal: Arthralgia, leg cramps, myalgia, paresthesia, rigors, weakness •  Otic: Earache, otitis media •  Respiratory: Coughing, pharyngitis, rhinitis, sinusitis •  Miscellaneous: Allergy, diaphoresis

  13. 1% to 4%: • Endocrine & metabolic: Hypoglycemia (2% to 4%), hypokalemia, hypoproteinemia, gout, cachexia, menstrual irregularities, breast pain, impotence •  Gastrointestinal: Colitis, diverticulitis, dysphagia, gastritis, gastroenteritis, gingivitis, glossitis, melena, stomatitis, taste perversion. • Cardiovascular: Angina, cardiac failure, cerebral vascular disorder, edema, flushing, hematoma, phlebitis, tachycardia • Central nervous system: Abnormal gait, amnesia, dysphonia, hallucinations, nervousness, neuralgia, neuropathy, somnolence, tremor, vertigo • Dermatologic: Acne, alopecia, bruising, cellulitis.

  14.   Genitourinary: Incontinence • Hematologic: Epistaxis •   Hepatic: Ascites, jaundice •   Local: Injection hematoma •  Skeletal: Hyperkinesia, hypertonia •   Ocular: Blurred vision, visual disturbance •   Otic: Tinnitus •   Renal: Albuminuria, renal abscess •   Respiratory: Bronchitis, pleural effusion, pneumonia, pulmonary embolism

  15. Contraindication & Precautions • CONTRAINDICATION: Hypersensitivity to octreotide or any component. • PRECAUTIONS — Patients must be monitored closely for biliary tract abnormalities, hypothyroidism, and glucose tolerance. • use with caution in patients with renal impairment and consider dosage modification in patients with severe renal failure requiring dialysis. • Chronic usage is associated with depressed vitamin B12 levels so we monitor it’s levels in patients receiving long-term therapy. • Monitor growth hormone in long-term therapy. • Pregnancy: class B

  16. Doses

  17. Doses • Dosage should be individualized according to the patient's response • Secretory diarrhea : I.V., SubQ: Doses of 1-10 mcg/kg every 12 hours have been used in children beginning at the low end of the range and increasing by 0.3 mcg/kg/dose at 3-day intervals. Suppression of growth hormone is of concern when used as long-term therapy. • Congenital hyperinsulinism: SubQ: Doses of 3-40 mcg/kg/day have been used.

  18. Acromegaly:  SubQ, I.V.: Initial: 50 mcg 3 times/day; titrate to achieve growth hormone levels <5 ng/mL or IGF-I (somatomedin C) levels <1.9 units/mL in males and <2.2 units/mL in females. Usual effective dose 100 mcg 3 times/day. Range 300-1500 mcg/day. • Note: Should be withdrawn yearly for a 4 week interval (8 weeks for depot injection) in patients who have received irradiation. Resume if levels increase and signs/symptoms recur. •   Continuous I.V. infusion rates have ranged from 25-50 mcg/hour for the treatment of esophageal variceal bleeding.

  19. Pharmacokinetics • After subcutaneous injection, octreotide is absorbed rapidly and completely from the injection site. Peak concentrations of 5.2 ng/mL (100 mcg dose) were reached 0.4 hours after dosing. • Using a specific radioimmunoassay, intravenous and subcutaneous doses were found to be bioequivalent. • The elimination of octreotide from plasma had an apparent half-life of 1.7 to 1.9 hours compared with 1-3 minutes with the natural hormone. • Metabolism: Extensive by the liver • Elimination: 32% excreted unchanged in urine

  20. Thank You

More Related