Clonidine HCl Actavis may be available in the countries listed below.
Clonidine hydrochloride (a derivative of Clonidine) is reported as an ingredient of Clonidine HCl Actavis in the following countries:
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Ciprolen may be available in the countries listed below.
Ciprofloxacin hydrochloride (a derivative of Ciprofloxacin) is reported as an ingredient of Ciprolen in the following countries:
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Gyno Myk may be available in the countries listed below.
Butoconazole nitrate (a derivative of Butoconazole) is reported as an ingredient of Gyno Myk in the following countries:
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Anti Kalium may be available in the countries listed below.
Polystyrene Sulfonic Acid calcium salt (a derivative of Polystyrene Sulfonic Acid) is reported as an ingredient of Anti Kalium in the following countries:
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Sertralin Winthrop may be available in the countries listed below.
Sertraline hydrochloride (a derivative of Sertraline) is reported as an ingredient of Sertralin Winthrop in the following countries:
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Generic Name: Doxycycline
Class: Skin and Mucous Membrane Agents, Miscellaneous
Chemical Name: 4 - (Dimethylamino) - 1,4,4a,5,5a,6,11,12a - octahydro - 3,5,10,12,12a - pentahydroxy - 6 - methyl - 1,11 - dioxo - 2 - naphthacenecarboxamide monohydrate
Molecular Formula: C22H24N2O8•H20
CAS Number: 17086-28-1
Semisynthetic tetracycline antibiotic.1
Available as 40-mg capsules (Oracea) containing 2 types of doxycycline beads (i.e., 30 mg as immediate-release beads and 10 mg as delayed-release beads).1
Treatment of inflammatory lesions (papules and pustules) associated with rosacea (acne rosacea).1
Safety and efficacy not established for treatment of the erythematous, telangiectatic, or ocular components of rosacea.1
The 40-mg capsules of doxycycline (Oracea) are not indicated for the treatment or prevention of bacterial infections or to reduce the number of or eliminate organisms associated with bacterial disease.1 (See Selection and Use of Anti-infectives under Cautions).
Administer orally in the morning, on an empty stomach, at least 1 hour before or 2 hours after a meal.1
Give with adequate amounts of fluid to reduce risk of esophageal irritation and ulceration.1
40 mg once daily in the morning.1
Efficacy of the 40-mg capsules of doxycycline (Oracea) not established beyond 16 weeks and safety not established beyond 9 months of therapy.1
Exceeding the dosage of doxycycline recommended for rosacea may increase the incidence of adverse effects (e.g., development of drug-resistant bacteria).1
No specific dosage recommendations at this time.1
Dosage adjustment not required.9
No specific dosage recommendations at this time.1
Known hypersensitivity to doxycycline or other tetracyclines.1
Animal studies indicate possible fetal toxicity (e.g., retardation of skeletal development) and embryotoxicity.1
Use not recommended in pregnant women.1 Avoid pregnancy during therapy.1 If pregnancy occurs, immediately discontinue and apprise of potential fetal hazard.1
Use not recommended for individuals of either gender who are attempting to conceive a child.1
Avoid use during tooth development (the last half of pregnancy, infancy, childhood up to 8 years of age); potential for permanent tooth discoloration and enamel hypoplasia.1
Tetracyclines form a stable calcium complex in any bone-forming tissue.1 Reversible decrease in fibula growth rate has occurred in premature infants receiving oral tetracyclines.1
Treatment with anti-infectives may permit overgrowth of clostridia.1 5 6 7 8 Consider Clostridium difficile-associated diarrhea and colitis (antibiotic-associated pseudomembranous colitis) if diarrhea develops and manage accordingly.1 5 6 7 8
Some mild cases of C. difficile-associated diarrhea and colitis may respond to discontinuance alone.1 5 6 7 8 Manage moderate to severe cases with fluid, electrolyte, protein supplementation, and appropriate anti-infective therapy (e.g., oral metronidazole or vancomycin) as clinically indicated.1 5 6 7 8
Tetracyclines have antianabolic effects and may increase BUN concentrations.1 This effect usually is not clinically important in patients with normal renal function; however, high serum tetracycline concentrations may result in azotemia, hyperphosphatemia, and acidosis in patients with impaired renal function.1 (See Renal Impairment under Cautions.)
Possible photosensitivity reaction (e.g., exaggerated sunburn reaction).1
Avoid unnecessary exposure to sunlight or artificial UV light (sunlamps, solariums).1
Doxycycline may result in overgrowth of nonsusceptible organisms, including fungi.1 If superinfection occurs, discontinue doxycycline and initiate appropriate therapy.1
Tetracyclines may increase the incidence of vaginal candidiasis.1 Use with caution in patients with a history of or predisposition to candidiasis.1
To reduce development of drug-resistant bacteria and maintain effectiveness of other antibacterials, use the 40-mg capsules of doxycycline (Oracea) only for the treatment of rosacea.1
Doxycycline 40-mg capsules are not to be used for the treatment or prevention of bacterial infections or to reduce or eliminate organisms associated with bacterial disease.1 The dosage regimen used for the treatment of rosacea results in doxycycline plasma concentrations that are too low for the treatment of bacterial infections.1
Tetracyclines have been associated with autoimmune syndromes (e.g., lupus-like syndrome, autoimmune hepatitis, vasculitis, serum sickness).1
If symptoms suggestive of an autoimmune syndrome develop (e.g., fever, rash, arthralgia, malaise), immediately discontinue use of tetracyclines and perform appropriate tests (liver function tests, ANA, CBC) to evaluate the patient.1
Tetracyclines are known to cause hyperpigmentation in many organs (e.g., nails, bone, skin, eyes, thyroid, visceral tissue, oral cavity, sclerae, and heart valves).1
Tetracyclines have been reported to cause bulging fontanels in infants and benign intracranial hypertension (pseudotumor cerebri) in adults.1 These effects usually resolve when the drug is discontinued.1
Periodically assess organ system function (including hematopoietic, renal, and hepatic function).1 Perform appropriate tests for autoimmune syndromes if indicated.1
Category D.1 (See Fetal/Neonatal Morbidity and Mortality under Cautions.)
Distributed into milk.1 Discontinue nursing or the drug.1
Safety and efficacy not established; use not recommended.1
Possible permanent tooth discoloration in children <8 years of age.1 (See Dental and Bone Effects under Cautions.) Do not use in infants or children <8 years of age.1
Serum half-life of doxycycline is not altered in patients with severe renal impairment;1 renal impairment does not appear to result in excessive accumulation of doxycycline.10 (See Renal Effects under Cautions.)
Excessive drug accumulation and possible liver toxicity may occur if usual dosages of some tetracyclines are used in patients with renal impairment.1 Dosage adjustment of tetracyclines may be necessary in patients with renal impairment; serum tetracycline concentrations should be monitored in patients receiving long-term therapy.1
Nasopharyngitis,1 hypertension,1 sinusitis,1 increased AST,1 upper respiratory tract infection,4 headache,4 diarrhea.4
Drug | Interaction | Comments |
|---|---|---|
Antacids (aluminum-, calcium- or magnesium- containing) | Decreased absorption of doxycycline1 | Give antacids containing aluminum, calcium, or magnesium 1–2 hours before or after doxycycline9 |
Anticoagulants, oral | Decreased plasma prothrombin activity1 | Monitor PT carefully; adjust anticoagulant dosage as needed1 |
Anticonvulsants (carbamazepine, barbiturates, phenytoin) | Possible decreased doxycycline half-life1 | |
Bismuth subsalicylate | Decreased absorption of doxycycline1 | If concomitant use cannot be avoided, give doxycycline at least 2-3 hours before bismuth subsalicylate9 |
Hormonal contraceptives | Decreased effectiveness of oral contraceptive1 | Use of a second form of contraceptive during treatment with doxycycline is advised1 |
Iron-containing preparations | Decreased absorption of doxycycline1 | Give doxycycline 2 hours before or 3 hours after iron-containing preparations9 |
Methoxyflurane (no longer commercially available in the US) | Fatal renal toxicity1 | |
Penicillins | Decreased efficacy of penicillins1 | Avoid concomitant use1 |
Proton-pump inhibitors | Decreased absorption of doxycycline1 | |
Retinoids, oral (e.g., acitretin, isotretinoin) | Additive adverse CNS effect of pseudotumor cerebri (benign intracranial hypertension)1 | Avoid concomitant use1 |
Urinary catecholamine assay | Possible false elevation secondary to interference with fluorescence test1 |
Oracea is not bioequivalent to other commercially available doxycycline preparations.1
Decreased rate and extent of absorption when administered with a high-fat, high-protein meal including dairy products.1
Bioavailability is reported to be reduced at high pH; may be clinically important in patients with gastrectomy, gastric bypass surgery, or those who otherwise are achlorhydric.1
Crosses the placenta and is distributed into milk.1
>90%.1
Major metabolites not identified.1
Excreted in urine (29–55% by 72 hours) and feces as unchanged drug.1
21 hours.1
No significant difference in serum half-life of patients with normal and severely impaired renal function.1 Hemodialysis does not alter the serum half-life.1
Tight, light-resistant containers at 15–30°C.1
Semisynthetic tetracycline antibiotic; also has anti-inflammatory and immunomodulatory effects.1 2 3
Mechanism(s) by which doxycycline reduces inflammatory lesions (papules and pustules) in patients with rosacea not known.2 Effects may result at least in part from the anti-inflammatory and antiangiogenic actions of the drug.2
The plasma concentrations of doxycycline achieved during therapy with the 40-mg capsules (Oracea) are less than the concentration required to treat bacterial diseases.1
Causes no long-term effects on bacterial flora of the oral cavity, skin, intestinal tract, or vagina.1
Importance of taking dose in the morning, on an empty stomach (at least 1 hour before or 2 hours after a meal) and drinking sufficient amounts of fluid to reduce the risk of esophageal irritation and ulceration.1 Importance of not lying down immediately following the dose.9
Importance of avoiding exposure to direct sunlight or UV light while taking doxycycline.1 When exposure cannot be avoided, importance of wearing protective clothing.1 Importance of discontinuing the drug and informing clinician at the first sign of skin erythema.1
Importance of taking only as prescribed; increasing dosage above 40 mg daily may increase the likelihood that bacteria will develop resistance and will not be treatable by other antibacterial drugs in the future.1
Importance of women using alternative nonhormonal contraceptive measures because of the potential interaction with hormonal contraceptives.1
Advise patients that autoimmune syndromes have been observed with doxycycline; importance of discontinuing the drug and informing clinician if arthralgia, fever, rash, or malaise occurs.1
Advise patients that doxycycline therapy can cause discoloration of skin, scars, teeth, or gums.1
Importance of providing patient a copy of manufacturer's patient information.1
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal supplements, as well as any concomitant diseases.1
Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed; necessity for clinicians to advise women to avoid pregnancy during therapy, advise pregnant women of risk to the fetus, and advise males to utilize effective contraception during therapy.1
Importance of informing patients of other important precautionary information. (See Cautions.)
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|---|---|---|---|
Oral | Capsules (containing beads) | 40 mg (immediate-release 30 mg with delayed-release 10 mg) | Oracea | CollaGenex |
This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.
The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.
AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions August 2008. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.
1. CollaGenex. Oracea (doxycycline, USP) capsules 40 mg prescribing information. Newtown, PA; 2006 May 26.
2. Sapadin AN, Fleischmajer R. Tetracyclines: nonantibiotic properties and their clinical implications. J Am Acad Dermatol. 2006; 54:258-65. [PubMed 16443056]
3. Anon. Low-dose doxycycline (Oracea) for rosacea. Med Lett Drugs Ther. 2007; 49:5-6.
4. Del Rosso JQ, Webster GF, Jackson M et al. Two randomized phase III clinical trials evaluating anti-inflammatory dose doxycycline (40-mg doxycycline, USP capsules) administered once daily for treatment of rosacea. J Am Acad Dermatol. 2007; 56:791-802. [PubMed 17367893]
5. Johnson S, Gerding DN. Clostridium difficile-associated diarrhea. Clin Infect Dis. 1998; 26:1027-36. [IDIS 407733] [PubMed 9597221]
6. Gerding DN, Johnson S, Peterson LR et al for the Society for Healthcare Epidemiology of America. Position paper on Clostridium difficile-associated diarrhea and colitis. Infect Control Hosp Epidemiol. 1995; 16:459-77. [PubMed 7594392]
7. Fekety R for the American College of Gastroenterology Practice Parameters Committee. Guidelines for the diagnosis and management of Clostridium difficile-associated diarrhea and colitis. Am J Gastroenterol. 1997; 92:739-50. [IDIS 386628] [PubMed 9149180]
8. American Society of Health-System Pharmacists Commission on Therapeutics. ASHP therapeutic position statement on the preferential use of metronidazole for the treatment of Clostridium difficile-associated disease. Am J Health-Syst Pharm. 1998; 55:1407-11. [IDIS 407213] [PubMed 9659970]
9. Collagenex, Newtown, PA: Personal communication.
10. Pfizer. Vibramycin calcium (doxycycline calcium) oral suspension syrup, Vibramycin hyclate (doxycycline hyclate) capsules, Vibramycin monohydrate (doxycycline monohydrate) for oral suspension, Vibra-tabs (doxycycline hyclate) film coated tablets prescribing information. New York, NY. 2003 Sep.
Class: Other Miscellaneous Therapeutic Agents
VA Class: GA208
Chemical Name: [R - (R*,R*)] - d - Phenylalanyl - l - cysteinyl - l - phenylalanyl - d - tryptophyl - l - lysyl - l - threonyl - N - [2 - hydroxy - 1 - (hydroxymethyl)propyl] - l - cysteinamide cyclic(2→7)-disulfide acetate (salt)
Molecular Formula: C49H66N10O10S2•× C2H4O2
CAS Number: 79517-01-4
Brands: Sandostatin, Sandostatin LAR Depot
Synthetic polypeptide structurally and pharmacologically related to somatostatin (growth hormone [somatropin] release inhibiting factor).1 2 3 4 5 7 20 26
Symptomatic treatment to suppress or inhibit severe diarrhea and flushing associated with carcinoid tumors.1 2 3 7 13 14 15 16
Long-acting suspension is used for long-term management of severe diarrhea and flushing episodes associated with metastatic carcinoid tumors in patients in whom initial treatment with octreotide immediate-release injection has been shown to be effective and tolerated (designated an orphan drug by FDA for this use).26 27
Acute management of potentially life-threatening hypotension associated with carcinoid crisis.1 2 3 7 11 12 14 15 17 19 20
Prophylaxis of carcinoid crisis that might be precipitated by anesthesia, surgery, initiation of chemotherapy, or infection.2 3 7 11 12 14 15 17 19 20
Management of profuse watery diarrhea associated with vasoactive intestinal polypeptide (VIP)-secreting tumors.1 2 3 7 12
Long-acting suspension is used for long-term management of profuse watery diarrhea associated with VIP-secreting tumors in patients who have been treated successfully with octreotide immediate-release injection (designated an orphan drug by FDA for this use).26 27
Treatment to reduce growth hormone (GH) and insulin-like growth factor I (IGF-I) blood concentrations in patients with acromegaly who have had inadequate responses to or are not candidates for surgical resection, pituitary irradiation, and bromocriptine mesylate (at maximally tolerated doses).1
Long-acting suspension is used for long-term therapy in patients who are candidates for medical therapy and who have been treated successfully with immediate-release injection (designated an orphan drug by FDA for this use).26 27 Long-acting suspension may be used in patients who are not candidates for surgery or who have had an inadequate response to surgery or patients who have had a suboptimal response to radiation therapy.26
Has been used in a limited number of neonates and infants to stabilize plasma glucose levels prior to pancreatectomy†, to treat recurrent post-operative hypoglycemia†, and as an alternative medical treatment to diazoxide for control of hypoglycemia†.1 3 26
Octreotide acetate is commercially available as an immediate-release injection for sub-Q or IV administration and as a long-acting suspension for IM administration.1 26
Clinical and/or biochemical response may diminish to some extent during prolonged therapy.7 14
Measurement of 5-HIAA (urinary 5-hydroxyindole acetic acid), plasma serotonin, or plasma Substance P may be useful in monitoring response to therapy.1 26
Measurement of VIP (plasma vasoactive intestinal peptide) may be useful in monitoring response to therapy.1 26
Measurement of growth hormone (GH) or insulin growth factor (IGF-I [somatomedin C]) may be useful in monitoring response to therapy.1 26
Administer immediate-release injection sub-Q or IV, as a rapid IV injection1 2 3 or as an IV infusion.1 2 3 7
Sub-Q injection is the usual route of administration because of delayed absorption and somewhat prolonged activity, as well as patient convenience.1 2 3 7
IV administration generally is reserved for emergency situations (e.g., acute management of carcinoid crisis) in which the drug can be injected rapidly.1 2
Administer long-acting suspension IM;26 do not administer sub-Q or IV.26
Administration of long-acting suspension at intervals >4 weeks is not recommended.26
Administer immediate-release injection between meals and at bedtime to minimize adverse GI effects; reducing dietary fat also may decrease adverse GI effects.3 7 11 (See Biliary Effects under Cautions.)
To minimize pain, administer smallest volume that will deliver the desired dose; rotate injection site systematically.1 2 Avoid multiple injections at the same site within short periods of time.1 2
Daily dosage may be given in 2–4 divided doses.1 21
Administer long-acting suspension IM into the gluteal muscle; alternate injection sites to minimize irritation.26 Injection into the deltoid muscle results in severe discomfort and is not recommended.26
IM administration of long-acting suspension may be used after tolerance established with at least 2 weeks of sub-Q therapy with immediate-release injection.26
Must be given under the supervision of a clinician.26
Reconstitute long-acting suspension immediately prior to administration.26
Prior to reconstitution, remove long-acting suspension kit from refrigerator and allow it to remain at room temperature for 30–60 minutes.26 Do not inject provided diluent without preparing long-acting suspension.26 Closely follow mixing instructions included in the packaging.26
For solution and drug compatibility information, see Stability: Compatibility.
Immediate-release injection may be diluted in 50–200 mL of 0.9% sodium chloride or 5% dextrose injection.1 10
Dilutions of immediate-release injection may be infused over 15–30 minutes.1 Alternatively, infuse over 8–24 hours.16
For solution and drug compatibility information, see Stability: Compatibility.
For rapid, direct IV injection (IV bolus), immediate-release injection may be administered undiluted.1 2 21
Direct IV administration is generally reserved for emergencies (e.g., acute management of carcinoid crisis).1 2
Immediate-release injection may be diluted in 50–200 mL of 0.9% sodium chloride or 5% dextrose injection and administered by IV push over 3 minutes.1 10
Available as octreotide acetate; dosage expressed in terms of octreotide.1 2 26
Usual dosages are not well defined because of the wide variation in disease severity and response.7 12
Individualize dosage according to patient response (symptomatic relief, biochemical response) and tolerance.1 2 3 7 12 14 16 19 26
Initiate therapy with immediate-release injection administered sub-Q.26 If patient responds well after ≥2 weeks of sub-Q therapy, switch to long-acting suspension administered IM.26
Maintain therapy with sub-Q injections of immediate-release injection for at least 2 weeks after initiating therapy with long-acting suspension.26
Dosages of 1–40 mcg/kg (immediate-release injection) daily have been used in neonates and infants to stabilize plasma glucose levels prior to pancreatectomy, to treat recurrent post-operative hypoglycemia, and as an alternative medical treatment to diazoxide for control of hypoglycemia;1 3 26 however, experience in pediatric patients is limited.1
Initially, 50–100 mcg (immediate-release injection) 1–3 times daily1 2 3 7 12 14 19 21 (usually 50 mcg 2 or 3 times daily).1 2 Subsequent dosage may be increased gradually according to patient response and tolerance.1 2 3 7 12 14 19
Initiate therapy with 100–600 mcg of immediate-release injection daily (average 300 mcg daily), given in 2–4 divided doses for at least 2 weeks.1 21 26
Median maintenance dosage (immediate-release injection) in clinical studies was approximately 450 mcg daily, clinical and biochemical benefits were obtained with as little as 50 mcg daily, dosages up to 1500 mcg daily sometimes were required; experience with dosages >750 mcg daily is limited.1 2
When switching to IM injection of long-acting suspension, continue sub-Q injections of immediate-release formulation at the previous dosage during at least the first 2 weeks of therapy with the long-acting suspension; sub-Q therapy (immediate-release injection) may be needed as long as 3–4 weeks to prevent exacerbation of disease symptoms.26
Temporary concomitant use of sub-Q therapy with immediate-release injection (at the dosage used prior to switching to the long-acting suspension) may be required to control exacerbation of symptoms that occur during IM therapy with long-acting suspension.26
Initially, 20 mg (long-acting suspension) once every 4 weeks for 2 months in patients who have responded well to ≥2 weeks of therapy with immediate-release injection.26 After 2 months of therapy, dosage may be increased to 30 mg once every 4 weeks if necessary for adequate symptom control.26 Dose may be decreased to 10 mg every 4 weeks if satisfactory symptom relief is achieved with the 20 mg dose.26
Safety and efficacy of doses >30 mg (long-acting suspension) have not been evaluated and are not recommended.26
Administer immediate-release injection by rapid IV injection13 17 19 20 or prolonged IV infusion.16
50–500 mcg (immediate-release injection) administered by rapid IV injection and repeated as necessary.13 17 19 20
Alternatively, 50 mcg/hour (immediate-release injection) infused IV for 8–24 hours.16
250–500 mcg (immediate-release injection) 1–2 hours prior to anesthetic induction has been used to prevent carcinoid crisis associated with surgery.13 19
150–250 mcg (immediate-release injection) every 6–8 hours 24–48 hours prior to anesthetic induction or initiation of chemotherapy has been used.13 19
Initiate therapy with 200–300 mcg of immediate-release injection daily given in 2–4 divided doses for at least 2 weeks.1 21 26
Dosages range from 150–750 mcg (immediate-release injection) daily during this period; >450 mcg daily usually not required.1 26
When switching to IM injection of long-acting suspension, continue sub-Q injections of immediate-release injection at the previous dosage during at least the first 2 weeks of therapy with the long-acting suspension; sub-Q therapy (immediate-release injection) may be needed as long as 3–4 weeks to prevent exacerbation of disease symptoms.26
Temporary concomitant use of sub-Q therapy with immediate-release injection (at the dosage used prior to switching to the long-acting suspension) may be required to control exacerbation of symptoms that occur during IM therapy with long-acting suspension.26
Initially, 20 mg (long-acting suspension) once every 4 weeks for 2 months in patients who have responded well to ≥2 weeks of therapy with immediate-release injection.26 After 2 months of therapy, increase dosage to 30 mg once every 4 weeks if necessary for adequate symptom control.26 Dose may be decreased to 10 mg every 4 weeks if satisfactory symptom relief is achieved with the 20 mg dose.26
Safety and efficacy of doses >30 mg (long-acting suspension) have not been evaluated and are not recommended.26
Initiate therapy with low dosage immediate-release injection administered sub-Q to promote tolerance to adverse GI effects during titration.1 26
Patients responding well to immediate-release injection (based on GH and IGF-I levels) and who tolerate the drug may be switched to the long-acting suspension administered IM.26
Initiate therapy with 150 mcg (immediate-release injection) daily given in 3 divided doses.1 26
Titrate dosage by tolerance, clinical effect, and evaluation of multiple GH levels.1 26 Adjust dosage based on GH levels measured at 1- to 4-hour intervals for 8–12 hours after sub-Q injection1 26 or alternatively, based on a single IGF-I level measured 2 weeks after initiation of therapy or a dosage change.1 26
300–600 mcg (immediate-release injection) daily given in 3 divided doses generally results in maximum effect; up to 1500 mcg daily given in 3 divided doses may be needed in some cases.1 26
If patient has received pituitary irradiation, withdraw therapy for approximately 4 weeks each year to assess disease activity.1 If GH or IGF-I levels increase and symptoms recur, resume therapy.1
Initially 20 mg (long-acting suspension) once every 4 weeks for 3 months in patients who have responded well to immediate-release injection.26
Subsequent doses of long-acting suspension are determined based on GH and IGF-I concentrations and clinical response.26 (See Table 1.)
GH and IGF-I measurements may be made after 3 monthly IM injections.26 Adjust dosage based on the mean of 4 GH levels measured at 1-hour intervals taken 4 weeks after the last injection of long-acting suspension or a single IGF-I level measured 4 weeks after the last injection of long-acting suspension.26
Growth Hormone (ng/mL) | Insulin Growth Factor (IGF-1) Concentration | Symptoms | Dosage |
|---|---|---|---|
≤2.5 | Normal | Controlled | 20 mg once every 4 weeks |
≤1 | Normal | Controlled | 10 mg once every 4 weeks |
>2.5 | Elevated | Uncontrolled | 30 mg once every 4 weeks |
If clinical and biochemical control is not obtained at a dosage of 30 mg once every 4 weeks, dosage may be increased to 40 mg once every 4 weeks; doses >40 mg are not recommended.26
If patient has received pituitary irradiation, withdraw therapy yearly for approximately 8 weeks to assess disease activity.26 If GH or IGF-I levels increase and symptoms recur, resume therapy.26
Maximum recommended dosage has not been established; however, dosages ≥5 times usual (e.g., 1500–3000 mcg daily) have been used,1 2 3 7 12 14 19 21 26 and substantially higher single doses (e.g., up to 120 mg infused IV over 8 hours) reportedly have been administered without serious adverse effect.1 2 26
Potential long-term effects (e.g., adverse GI and biliary effects) of relatively high dosages have not been fully elucidated.1 2 19 Possibility that clinical and/or biochemical response may diminish to some extent during prolonged therapy should be considered.7 14
Limited experience with daily dosages exceeding 750 mcg (immediate-release injection); dosages up to 1500 mcg daily have been used.1 2
Safety and efficacy of doses >30 mg (long-acting suspension) have not been evaluated and are not recommended.26
Safety and efficacy of doses >30 mg (long-acting suspension) have not been evaluated and are not recommended.26
Doses >40 mg (long-acting suspension) are not recommended.26
Clearance may be reduced substantially in patients with severe renal impairment; dosage reduction may be necessary in patients with renal failure requiring dialysis.1 2 26
Elimination may be prolonged; dosage adjustment may be necessary.1 2 26
Known hypersensitivity to octreotide or any ingredient in the formulation.1 2 26
Biliary abnormalities (e.g., cholelithiasis, microlithiasis, sediment, sludge, and dilatation) occur commonly, 1 2 26 possibly due to drug-induced alterations in GI fat absorption, inhibited gallbladder contractility,1 2 6 12 26 and decreased bile secretion.1 26 Acute cholecystitis, ascending cholangitis, biliary obstruction, cholestatic hepatitis, and pancreatitis have been reported rarely.1 26 Incidence related to duration of therapy; incidence not apparently related to age, sex, or dose.1 26
If severe abdominal pain develops during therapy, consider the possibility of biliary complications (e.g., cholelithiasis) potentially requiring surgical intervention.2
Anaphylaxis and anaphylactoid reactions have been reported.1 26
Monitor closely all patients with growth hormone secreting tumors; tumor expansion may result in serious complications (e.g., visual field defects).26
Hypoglycemia or hyperglycemia can occur as a result of altered balance between the counter-regulatory hormones (e.g., insulin, glucagon, growth hormone).1 2 3 6 7 12 26 Hypoglycemia, sometimes severe, more commonly occurs in patients with type I diabetes mellitus.1 26 Hyperglycemia more commonly occurs in nondiabetic patients and those with type II diabetes mellitus.1 26 Dosage adjustment may be required for insulin or hypoglycemic agents in patients with diabetes mellitus.1 2 6 12 26
Monitor glucose tolerance and antidiabetic treatment periodically.1 26
Hypothyroidism may result from suppression of secretion of thyroid stimulating hormone (TSH).1 2 26 Perform baseline and periodic assessment of thyroid function (e.g., TSH, total and/or free thyroxine [T4]).1 2 26 Patients with preexisting thyroid dysfunction may require adjustment in thyroid supplementation.3
Sinus bradycardia, conduction abnormalities, and arrhythmias reported in patients with acromegaly or carcinoid syndrome.1 26 ECG changes (e.g., QT prolongation, axis shifts, early repolarization, low voltage, R/S transition, early R-wave progression, and nonspecific ST-T-wave changes) and worsening of CHF reported.1 26 Dose adjustments in drugs with bradycardic effects (e.g., β-adrenergic blocking agents) may be required.1 26 (See Specific Drugs under Interactions.)
Decreases in serum vitamin B12 concentrations and abnormal Shilling’s test results reported; monitor vitamin B12 concentrations.1 26
Alterations in GI absorption of dietary fats reported.1 2 12 26
Consider possible interference with GI absorption of fat-soluble vitamins.2 3 7 12
Excessive increases in serum zinc concentrations may occur if octreotide is used to reduce excessive fluid loss from the GI tract in patients with conditions producing such a loss.26 Periodic monitoring of zinc levels is recommended in patients with this condition who are receiving concomitant total parenteral nutrition (TPN) and octreotide.26 (See Specific Drugs under Interactions.)
Up to 25% of patients develop antibodies to octreotide.1 26
Antibodies to octreotide do not affect clinical response; some evidence from clinical studies indicates that antibodies to octreotide may be associated with prolonged duration of GH suppression.26
Category B.1 26
Not known whether octreotide is distributed into milk.1 26 Caution if used in nursing women.1 26
Safety and efficacy of immediate-acting injection not established.1
Immediate-release injection has been used in a limited number of neonates and infants with congenital hyperinsulinism†.1 26 Adverse effects mainly involved the GI tract (e.g., steatorrhea, diarrhea, vomiting, abdominal distension).1 26 Poor growth, poor weight gain, and tachyphylaxis reported; “catch up” growth followed drug discontinuance.1 26 Potential effects of long-term therapy on pediatric growth and development not fully elucidated.3
Safety and efficacy of long-acting suspension formulation not established.26
Long-acting suspension investigated in pediatric patients 6–17 years of age with hypothalamic obesity† secondary to cranial insult; new cholelithiasis reported in 33% of children.26
Insufficient experience in patients ≥65 years of age to determine whether they respond differently than younger adults.1 26 Select dosage with caution because of age-related decreases in hepatic, renal, and/or cardiac function and potential for concomitant disease and drug therapy.1 26
Prolonged clearance and elimination half-life.1 2 26
Prolonged elimination and decreased clearance of immediate-release injection in patients with liver cirrhosis.1 Prolonged elimination in patients with fatty liver disease.1
Long-acting suspension formulation has not been studied in patients with hepatic impairment.26
Half-life of immediate-release injection increased.1 26 Dosage adjustment may be necessary in patients with renal failure requiring dialysis.26
Long-acting suspension formulation has not been studied in patients with renal impairment.26
Diarrhea, abdominal pain/discomfort, flatulence, fatty stools (including steatorrhea), nausea, vomiting, gallbladder and biliary tract abnormalities (cholelithiasis, sludge), sinus bradycardia, conduction abnormalities, arrhythmias, and local effects (pain, burning) at the injection site.1 2 3 7 12 26
Associated with alterations in nutrient absorption; may affect absorption of orally administered drugs.1 26
May inhibit CYP3A4 isoenzymes secondary to suppression of growth hormone.1 26
Octreotide may inhibit clearance of drugs metabolized by CYP3A4.1 26
Drug | Interaction | Comments |
|---|---|---|
Agents to control fluid and electrolyte balance | Possible alterations in fluid and electrolyte balance1 26 | Possible dosage adjustment1 26 |
Bromocriptine | Increased AUC of bromocriptine1 26 a | |
Cardiovascular agents with bradycardic effects (β-adrenergic blocking agent, calcium-channel blocking agent) | Potential additive bradycardic effect1 26 | Possible dosage adjustment1 26 |
Cyclosporine | Possible decreased plasma cyclosporine concentrations and transplant rejection1 26 | |
Insulin | Inhibits insulin; possible alterations of plasma glucose levels (hypoglycemia or hyperglycemia)1 26 | Possible dosage adjustment1 26 |
Oral hypoglycemic agents | Inhibits insulin; possible alterations of plasma glucose levels (hypoglycemia or hyperglycemia)1 26 | Possible dosage adjustment1 26 |
Quinidine | Possible decreased quinidine clearance1 26 | Use concomitantly with caution1 26 |
Total parenteral nutrition | Possible excessive increases of serum zinc when the fluid loss is reversed26 | Monitor zinc levels during concomitant TPN and octreotide therapy in patients receiving octreotide to reduce excessive fluid loss from the GI tract26 (See GI Effects under Cautions) |
Following sub-Q injection, immediate-release formulation is rapidly and completely absorbed; peak concentrations are attained in 0.4 hours.1 26 Sub-Q and IV doses of immediate-release formulation are bioequivalent.1 26
After IM administration of the long-acting suspension, peak plasma concentration is attained initially within 1 hour, progressively declines to a nadir within 3–5 days, and then slowly increases to a dose proportional peak concentration about 2–3 weeks post injection.26
The relative bioavailability of the long-acting suspension given IM compared to the immediate-release injection given sub-Q is 60–63%.26 Following multiple IM injections of long-acting suspension given every 4 weeks, steady-state octreotide concentrations are achieved after the third injection.26 e
Duration of action of immediate-release injection is variable but extends up to 12 hours depending upon the type of tumor.1 26
Following administration of long-acting suspension, plateau plasma concentrations are maintained over a period of 2–3 weeks.26
In patients with acromegaly, the time to peak plasma concentration is 0.7 hours following administration of immediate-release formulation.1 26
Steady-state volume of distribution is about 13.6 L.1 26 Distribution into erythrocytes appears negligible.1 26 It is not known whether the drug is distributed into breast milk.1 26
Approximately 65% bound to plasma proteins, mainly to lipoprotein and, to a lesser extent, albumin.1 26
In patients with acromegaly, the steady-state volume of distribution is about 21.6 L and the plasma protein binding is 41.2%.1 26
Approximately 32% excreted in urine as unchanged drug.1 26
Apparent elimination half-life is 1.7–1.9 hours.1 26
Following administration of the immediate-release injection, elimination half-life of 2.4, 3, or 3.1 hours reported in patients with mild renal impairment (Clcr 40–60 mL/minute), moderate impairment (Clcr 10–39 mL/minute), or severe impairment (Clcr <10 mL/minute), respectively.1
In patients with severe renal failure requiring dialysis, clearance of immediate-release injection is decreased by approximately 50% compared with healthy individuals.1 26 (See Special Populations under Dosage and Administration.)
Long-acting suspension has not been studied in patients with renal or hepatic impairment.26
Elimination of immediate-release injection prolonged in patients with liver cirrhosis; half-life increased to 3.7 hr.1 Half-life increased to 3.4 hr in patients with fatty liver disease.1
In geriatric individuals, the half-life is prolonged by 46%, and the clearance is decreased by 26%.1 26
In patients with acromegaly, disposition and elimination half-life of the drug are similar to healthy individuals.1 26
2–8°C; protect from light.1 10
May store at 20–30°C for up to 14 days if protected from light.1 21 25
May allow to come to room temperature before administration; do not warm artificially.1
Open ampuls just prior to administration; discard unused drug.1
Diluted solutions are stable for ≥24 hours.1 10
2–8°C; protect from light.26
Product kit should remain at room temperature for 30–60 minutes before preparation of the suspension.26
For information on systemic interactions resulting from concomitant use, see Interactions.
Incompatible in total parenteral nutrition solutions; formation of a glycosyl octreotide conjugate may decrease octreotide efficacy.1
Compatible |
|---|
Sodium chloride 0.9% |
Incompatible |
Fat emulsion 10%, IV |
Compatible |
|---|
Heparin sodium |
Variable |
|---|
Pantoprazole sodium |
Inhibits secretion of anterior pituitary hormones, suppresses pancreatic endocrine and exocrine function, inhibits gastric acid and GI hormone secretion, suppresses serotonin secretion, inhibits GI motility and splanchnic blood flow, and alters GI absorption.1 2 3 4 5 6 7 8 26
More potent than somatostatin, inhibits somatropin release to a greater extent than insulin and glucagon release, and has a longer plasma half-life and duration of action relative to somatostatin.1 2 3 4 7 19 26
Suppresses somatropin secretion and the lutropin (luteinizing hormone) response to gonadotropin-releasing hormone (GnRH).1 2 26
Has been used to control GI and other manifestations of a variety of conditions (e.g., flushing and diarrhea associated with carcinoid syndrome, watery diarrhea associated with VIP-secreting tumors) because of its inhibitory effects on secretion of serotonin and various gastroenteropancreatic peptides (e.g., gastrin, vasoactive intestinal polypeptide [VIP], insulin, glucagon, secretin, motilin, pancreatic polypeptide).1 2 3 4 6 7 8 12 14 15 16 17 18 19 20 26
Decreases the concentration of growth hormone and/or insulin-like growth factor I (IGF-I, somatomedin C) in patients with acromegaly.1 26
Importance of instructing patient and/or caregiver regarding sterile sub-Q injection technique.1 2 14
Importance of advising patients with carcinoid tumors or vasoactive intestinal polypeptide-secreting tumors to closely follow return visit reinjection schedule in order to minimize exacerbation of symptoms.26
Importance of advising patients with acromegaly to closely follow return visit reinjection schedule in order to maintain steady control of GH and IGF-1 levels.26
Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1 26
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.1 26
Importance of informing patients of other important precautionary information.1 26 (See Cautions.)
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|---|---|---|---|
Parenteral | Injection | 50 mcg (of octreotide) per mL | Sandostatin (preservative-free ampuls) | Novartis |
Octreotide Injection | APP, Bedford , Teva | |||
Definition of Nosocomial Pneumonia: An infection of the lungs contracted during a hospital stay.
The following drugs and medications are in some way related to, or used in the treatment of Nosocomial Pneumonia. This service should be used as a supplement to, and NOT a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners.
Nifédipine Sandoz may be available in the countries listed below.
Nifedipine is reported as an ingredient of Nifédipine Sandoz in the following countries:
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