Octreotide

Brand names: Sandostatin LAR®Sandostatin®

Chemical formula:

Drug Forms:
• Octreotide Acetate Solution for injection (below)
• Octreotide Acetate Suspension for injection

Español:
• Acetato de octreotida, Solución para inyección
• Acetato de octreotida, Suspensión para inyección

Octreotide Acetate Solution for injection

What is this medicine?

OCTREOTIDE (ok TREE oh tide) is used to reduce blood levels of growth hormone in patients with a condition called acromegaly. This medicine also reduces flushing and watery diarrhea caused by certain types of cancer.
 
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
•gallbladder disease
•kidney disease
•liver disease
•an unusual or allergic reaction to octreotide, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding

How should I use this medicine?

This medicine is for injection under the skin or into a vein (only in emergency situations). It is usually given by a health care professional in a hospital or clinic setting.

If you get this medicine at home, you will be taught how to prepare and give this medicine. Allow the injection solution to come to room temperature before use. Do not warm it artificially. Use exactly as directed. Take your medicine at regular intervals. Do not take your medicine more often than directed.

It is important that you put your used needles and syringes in a special sharps container. Do not put them in a trash can. If you do not have a sharps container, call your pharmacist or healthcare provider to get one.

Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.

What may interact with this medicine?

Do not take this medicine with any of the following medications:
•cisapride
•droperidol
•general anesthetics
•grepafloxacin
•perphenazine
•thioridazine

This medicine may also interact with the following medications:
•bromocriptine
•cyclosporine
•diuretics
•medicines for blood pressure, heart disease, irregular heart beat
•medicines for diabetes, including insulin
•quinidine

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Visit your doctor or health care professional for regular checks on your progress.

To help reduce irritation at the injection site, use a different site for each injection and make sure the solution is at room temperature before use.

This medicine may cause increases or decreases in blood sugar. Signs of high blood sugar include frequent urination, unusual thirst, flushed or dry skin, difficulty breathing, drowsiness, stomach ache, nausea, vomiting or dry mouth. Signs of low blood sugar include chills, cool, pale skin or cold sweats, drowsiness, extreme hunger, fast heartbeat, headache, nausea, nervousness or anxiety, shakiness, trembling, unsteadiness, tiredness, or weakness. Contact your doctor or health care professional right away if you experience any of these symptoms.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:
•allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
•changes in blood sugar
•changes in heart rate
•severe stomach pain

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•diarrhea or constipation
•gas or stomach pain
•nausea, vomiting
•pain, redness, swelling and irritation at site where injected

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medicine?

Keep out of the reach of children.

Store in a refrigerator between 2 and 8 degrees C (36 and 46 degrees F). Protect from light. Allow to come to room temperature naturally. Do not use artificial heat. If protected from light, the injection may be stored at room temperature between 20 and 30 degrees C (70 and 86 degrees F) for 14 days. After the initial use, throw away any unused portion of a multiple dose vial after 14 days. Throw away unused portions of the ampules after use.

Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

A somatostatin analog used in the treatment of endocrine disorders of the pituitary and pancreas.

Octreotide
Systematic (IUPAC) name
(4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-19- [[(2R)-2-amino-3-phenyl-propanoyl]amino]-16- benzyl-N-[(2R,3R)-1,3-dihydroxybutan-2-yl]-7- (1-hydroxyethyl)-13-(1H-indol-3-ylmethyl)-6,9,12, 15,18-pentaoxo-1,2-dithia-5,8,11,14,17- pentazacycloicosane-4-carboxamide
Identifiers
CAS number	83150-76-9
ATC code	H01CB02
PubChem	54373
DrugBank	BTD00088
Chemical data
Formula	C49H66N10O10S2
Mol. mass	1019.24 g/mol
Pharmacokinetic data
Bioavailability	100%; I.M: 60% to 63% of subcutaneous dose
Protein binding	65%
Metabolism	Hepatic
Half life	1.7-1.9 hours
Excretion	?
Therapeutic considerations
Pregnancy cat.	B(US)
Legal status
Routes	Intramuscular, intravenous

Octreotide (brand name Sandostatin, Novartis Pharmaceuticals) is an octapeptide that mimics natural somatostatin pharmacologically, though it is a more potent inhibitor of growth hormone, glucagon, and insulin than the natural hormone. It was first synthesized in 1979 by the chemist Wilfried Bauer.

Contents 1 Pharmacological Effects 2 Adverse Effects 3 Uses 4 References 5 External links

Pharmacological Effects

Since octreotide resembles somatostatin in physiological activities, it can:

• Inhibit secretion of many hormones, such as gastrin, cholecystokinin, glucagon, growth hormone, insulin, secretin, pancreatic polypeptide, TSH, and vasoactive intestinal peptide.
• Reduce secretion of fluids by the intestine and pancreas.
• Reduce gastrointestinal motility and inhibit contraction of the gallbladder.
• Inhibit the action of certain hormones from the anterior pituitary.
• Cause vasoconstriction in the blood vessels.
• Reduce portal vessel pressures in bleeding varices
• It has also been shown to produce analgesic effects, most probably acting as a partial agonist at the mu opioid receptor.^[1][2]

Adverse Effects

Most Frequent Adverse Effects: Abdominal pain with cramps, bradycardia, cardiac conduction changes, gastrointestinal reactions (including nausea/vomiting and diarrhea or constipation), injection site reactions, nausea, vomiting

Less Frequent Adverse Effects: Discolored feces, dyspepsia, flatulence, hypothyroidism, steatorrhea, tenesmus

Rare Adverse Effects: Acute pancreatitis, alopecia, biliary calculi, liver failure, dizziness, edema, fatigue, fever, flushing, generalized weakness, headache, hepatitis, hyperbilirubinemia, hyperglycemia, prolonged QT interval

Uses

The Food and Drug Administration (FDA) has approved the usage of a salt form of this peptide, octreotide acetate, as an injectable depot formulation for the treatment of acromegaly, the treatment of diarrhea and flushing episodes associated with carcinoid syndrome, and treatment of diarrhea in patients with vasoactive intestinal peptide-secreting tumors (VIPomas).

Octreotide has also been used off-label for the treatment of severe, refractory diarrhea from other causes. It is used in toxicology for the treatment of prolonged recurrent hypoglycemia after sulfonylurea and possibly meglitinides overdose.

Octreotide has also been used with varying degrees of success in infants with nesidioblastosis to help decrease insulin hypersecretion.

In patients with suspected esophageal varices, octreotide can be given to help decrease bleeding.^[3]

Octreotide has been investigated for patients with pain from chronic pancreatitis.^[4]

Octreotide may be useful in the treatment of thymic neoplasms.

Octreotide has been used as an unlicensed drug, injected sub-cutaneously in the management of hypertrophic pulmonary osteoarthropathy (HPOA), secondary to non-small cell lung carcinoma. Although its mechanism is not known it appears to reduce the pain associated with HPOA

It has been used in the treatment of malignant bowel obstruction.^[5]

Octreotide may be used in conjunction with midodrine to partially reverse peripheral vasodilation in the hepato-renal syndrome. By increasing systemic vascular resistance, these drugs reduce shunting and improve renal perfusion, prolonging survival until definitive treatment with liver transplant. ^[6]

In recent years, the drug has been shown to be effective in the treatment of chylothorax.^[7][8]

References

1. ^ Maurer R, Gaehwiler BH, Buescher HH, Hill RC, Roemer D. Opiate antagonistic properties of an octapeptide somatostatin analog. Proceedings of the National Academy of Sciences USA. 1982 Aug;79(15):4815-7. PMID 6126877
2. ^ Allen MP, Blake JF, Bryce DK, Haggan ME, Liras S, McLean S, Segelstein BE. Design, synthesis and biological evaluation of 3-amino-3-phenylpropionamide derivatives as novel mu opioid receptor ligands. Bioorganic and Medicinal Chemistry Letters. 2000 Mar 20;10(6):523-6. PMID 10741545
3. ^ Abid S, Jafri W, Hamid S, et al. (March 2009). "Terlipressin vs. octreotide in bleeding esophageal varices as an adjuvant therapy with endoscopic band ligation: a randomized double-blind placebo-controlled trial". Am. J. Gastroenterol. 104 (3): 617–23. doi:10.1038/ajg.2008.147. PMID 19223890. http://dx.doi.org/10.1038/ajg.2008.147. 
4. ^ Uhl W, Anghelacopoulos SE, Friess H, Büchler MW (1999). "The role of octreotide and somatostatin in acute and chronic pancreatitis". Digestion 60 Suppl 2: 23–31. doi:10.1159/000051477. PMID 10207228. 
5. ^ Shima Y, Ohtsu A, Shirao K, Sasaki Y (May 2008). "Clinical efficacy and safety of octreotide (SMS201-995) in terminally ill Japanese cancer patients with malignant bowel obstruction". Japanese journal of clinical oncology 38 (5): 354–9. doi:10.1093/jjco/hyn035. PMID 18490369. http://jjco.oxfordjournals.org/cgi/pmidlookup?view=long&pmid=18490369. 
6. ^ Skagen C, Einstein M, Lucey MR, Said A (Feb 2009). "Combination Treatment With Octreotide, Midodrine, and Albumin Improves Survival in Patients With Type 1 and Type 2 Hepatorenal Syndrome.". J Clin Gastroenterol.. PMID 19238094. 
7. ^ Dalokay Kilic, MD, Ekber Sahin, MD, Oner Gulcan, MD, Bulent Bolat, MD, Riza Turkoz, MD, Ahmet Hatipoglu, MD (2005). "Octreotide for Treating Chylothorax after Cardiac Surgery". Texas Heart Institute Journal 32 (3): 437-39. http://www.pubmedcentral.nih.gov/picrender.fcgi?artid=1336729&blobtype=pdf. 
8. ^ Marcia L. Buck, Pharm.D., FCCP (2004). "Octreotide for the Management of Chylothorax in Infants and Children". Pediatric Pharmacotherapy 10 (10). http://www.medscape.com/viewarticle/494653. 

External links

• www.AcromegalyCommunity.com: Emotional and communal support for those touched by Acromegaly- page discussing drug, side effects, and prescription programs
• Caring for Carcinoid Foundation
• Sandostatin (Octreotide) brand homepage
• [1] Indevus Pharma and Octreotide

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