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Endocrine / Other
bromocriptine (Parlodel ® )
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INDICATIONS: Amenorrhea with or
without galactorrhea; infertility or hypogonadism; prolactin-secreting
adenomas; acromegaly; Parkinson's disease. Mechanism of Action Semisynthetic ergot alkaloid derivative and a dopamine receptor agonist which activates postsynaptic dopamine receptors in the tuberoinfundibular and nigrostriatal pathways DOSING - Adults: Parkinsonism: 1.25 mg 2 times/day, increased by 2.5 mg/day in 2- to 4-week intervals (usual dose range is 30-90 mg/day in 3 divided doses), though elderly patients can usually be managed on lower doses Neuroleptic malignant syndrome: 2.5-5 mg 3 times/day Hyperprolactinemia: 2.5 mg 2-3 times/day Acromegaly: Initial: 1.25-2.5 mg increasing as necessary every 3-7 days; usual dose: 20-30 mg/day Prolactin-secreting adenomas: Initial: 1.25-2.5 mg/day; may be increased as tolerated every 2-7 days until optimal response (range: 2.5-15 mg/day) Supplied: Capsule: 5 mg. Tablet: 2.5 mg |
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cabergoline (Dostinex ® )
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Long acting dopamine receptor agonist with a high affinity for D2
receptor. Dosing (Adults): Hyperprolactinemic disorders: Initial dose: 0.25 mg orally twice weekly. The dose may be increased by 0.25 mg twice weekly up to a maximum of 1 mg twice weekly according to the patient's serum prolactin level. Dosage increases should not occur more rapidly than every 4 weeks. Once a normal serum prolactin level is maintained for 6 months, the dose may be discontinued and prolactin levels monitored to determine if cabergoline is still required. The durability of efficacy beyond 24 months of therapy has not been established. Supplied: 0.5 mg tab. |
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calcitonin (Calcimar ® )
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INDICATIONS Calcitonin (salmon):
Treatment of Paget's disease of bone (osteitis deformans); adjunctive
therapy for hypercalcemia; used in postmenopausal osteoporosis and
osteogenesis imperfecta Mechanism of Action Structurally similar to human calcitonin; it directly inhibits osteoclastic bone resorption; promotes the renal excretion of calcium, phosphate, sodium, magnesium and potassium by decreasing tubular reabsorption; increases the jejunal secretion of water, sodium, potassium, and chloride DOSING - Adults: Paget's disease: I.M., SubQ: Initial: 100 units/day; maintenance: 50 units/day or 50-100 units every 1-3 days Hypercalcemia: Initial: I.M., SubQ: 4 units/kg every 12 hours; may increase up to 8 units/kg every 12 hours to a maximum of every 6 hours Osteogenesis imperfecta: I.M., SubQ: 2 units/kg 3 times/week Postmenopausal osteoporosis: I.M., SubQ: 100 units/day Intranasal: 200 units (1 spray)/day Administration I.M. route is preferred if volume exceeds 2 mL. Supplied Injection, solution, calcitonin-salmon: 200 int. units/mL (2 mL) Solution, nasal spray, calcitonin-salmon: 200 int. units/0.09 mL (3.7 mL) [contains benzalkonium chloride] |
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cinacalcet (Sensipar ® )
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MOA: Increases the sensitivity of the calcium-sensing
receptor on the parathyroid gland. Dosing (Adults): Secondary hyperparathyroidism: Initial: 30 mg orally once daily (maximum daily dose: 180 mg). Increase dose incrementally (60 mg, 90 mg, 120 mg, 180 mg once daily) as necessary to maintain iPTH level between 150-300 pg/mL. Note: Do not titrate dose more frequently than every 2-4 weeks. Parathyroid carcinoma: Initial: 30 mg orally twice daily (maximum daily dose: 360 mg daily as 90 mg 4 times/day). Increase dose incrementally (60 mg twice daily, 90 mg twice daily, 90 mg 4 times/day) as necessary to normalize serum calcium levels. REFERENCE RANGE — Chronic kidney disease: Goal iPTH: 150-300 pg/mL. Supplied: Tablet: 30 mg, 60 mg, 90 mg. |
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cosyntropin (Cortrosyn ®)
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Exhibits the full cortico-steroidogenic activity of natural ACTH MOA: Stimulates the adrenal cortex to secrete adrenal steroids (including hydrocortisone, cortisone), androgenic substances, and a small amount of aldosterone. INTRO: Severe hypofunction of the pituitary - adrenal axis is usually associated with subnormal plasma cortisol values but a low basal level is not per se evidence of adrenal insufficiency and does not suffice to make the diagnosis. Many patients with proven insufficiency will have normal basal levels and will develop signs of insufficiency only when stressed. For this reason a criterion which should be used in establishing the diagnosis is the failure to respond to adequate corticotropin stimulation. When presumptive adrenal insufficiency is diagnosed by a subnormal CORTROSYN test, further studies are indicated to determine if it is primary or secondary. Dosing (Adults): IM: Reconstitute 0.25 mg (250 mcg) with 1mL NS and inject intramuscularly. OR IV: Dilute in 2 to 5 mL of saline and give over a 2-minute period. The usual normal response in most cases is an approximate doubling of the basal level, provided that the basal level does not exceed the normal range. Diagnosis of adrenocortical insufficiency: IM, IV (over 2 minutes): Peak plasma cortisol concentrations usually occur 45-60 minutes after cosyntropin administration: 0.25 to 0.75 mg. Note: When greater cortisol stimulation is needed, an I.V. infusion may be used: 0.25 mg administered at 0.04 mg/hour over 6 hours. Normal response: Many patients with normal adrenal function, however, do not respond to the expected degree so that the following criteria have been established to denote a normal response:
ADDITIONAL INFO: Primary adrenal insufficiency (Addison’s disease) is the result of an intrinsic disease process, such as tuberculosis within the gland. The production of adrenocortical hormones is deficient despite high ACTH levels (feedback mechanism). Secondary or relative insufficiency arises as the result of defective production of ACTH leading in turn to disuse atrophy of the adrenal cortex. It is commonly seen, for ex-ample, as result of corticosteroid therapy, Sheehan’s syndrome and pituitary tumors or ablation. The differentiation of both types is based on the premise that a primarily defective gland cannot be stimulated by ACTH whereas a secondarily defective gland is potentially functional and will respond to adequate stimulation with ACTH. Patients selected for further study as the result of a subnormal CORTROSYNTM test should be given a 3 or 4 day course of treatment with Repository Corticotropin Injection USP and then retested. Suggested doses are 40 USP units twice daily for 4 days or 60 USP units twice daily for 3 days. Under these conditions little or no increase in plasma cortisol levels will be seen in Addison’s disease whereas higher or even normal levels will be seen in cases with secondary adrenal insufficiency. Supplied: Inj (powder for reconstitution): 0.25 mg |
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desmopressin (DDAVP ®)
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INDICATIONS Treatment of diabetes insipidus; control of bleeding in hemophilia A, and mild-to-moderate classic von Willebrand disease (type I); primary nocturnal enuresis Mechanism of Action Enhances reabsorption of water in the kidneys by increasing cellular permeability of the collecting ducts; possibly causes smooth muscle constriction with resultant vasoconstriction; raises plasma levels of von Willebrand factor and factor VIII Children >/= 12 years and Adults: Diabetes insipidus: I.V., SubQ: 2-4 mcg/day (0.5-1 mL) in 2 divided doses or 1 /10 of the maintenance intranasal dose Intranasal (using 100 mcg/mL nasal solution): 10-40 mcg/day (0.1-0.4 mL) divided 1-3 times/day; adjust morning and evening doses separately for an adequate diurnal rhythm of water turnover. Note: The nasal spray pump can only deliver doses of 10 mcg (0.1 mL) or multiples of 10 mcg (0.1 mL); if doses other than this are needed, the rhinal tube delivery system is preferred. Oral: Initial: 0.05 mg twice daily; total daily dose should be increased or decreased as needed to obtain adequate antidiuresis (range: 0.1-1.2 mg divided 2-3 times/day) Hemophilia A and mild to moderate von Willebrand disease (type I): I.V.: 0.3 mcg/kg by slow infusion, begin 30 minutes before procedure IIntranasal: Using high concentration spray (1.5 mg/mL): <50 kg: 150 mcg (1 spray); >50 kg: 300 mcg (1 spray each nostril); repeat use is determined by the patient's clinical condition and laboratory work; if using preoperatively, administer 2 hours before surgery Decrease bleeding following cardiac bypass: 0.3 mcg/kg ivpb. Provide short term protection for uremic hemorrhagic tendency: 0.3 mcg/kg ivpb q8h x 2 doses (diminishing response). PHARMACODYNAMICS / KINETICS Greatly enhanced ADH activity. Less vasopressor activity. Longer DOA. (Synthetic analog of vasopressin-posterior pituitary hormone). ADH activity : Pressor activity [DDAVP: 2000-4000: 1 Vasopressin: 1:1] |
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Leuprolide (Lupron ®)
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Gonadotropin Releasing Hormone Agonist. INDICATIONS Palliative treatment of advanced prostate carcinoma; management of endometriosis as initial treatment and/or treatment of recurrent symptoms; preoperative treatment of anemia caused by uterine leiomyomata (fibroids); central precocious puberty Mechanism of Action Potent inhibitor of gonadotropin secretion; continuous daily administration results in suppression of ovarian and testicular steroidogenesis due to decreased levels of LH and FSH with subsequent decrease in testosterone (male) and estrogen (female) levels. Leuprolide may also have a direct inhibitory effect on the testes, and act by a different mechanism not directly related to reduction in serum testosterone. Dosing (Adults): Advanced prostatic carcinoma: SubQ: Eligard®: 7.5 mg monthly or 22.5 mg every 3 months or 30 mg every 4 months Lupron®: 1 mg/day Viadur®: 65 mg implanted subcutaneously every 12 months I.M.: Lupron Depot®: 7.5 mg/dose given monthly (every 28-33 days) or Lupron Depot-3®: 22.5 mg every 3 months or Lupron Depot-4®: 30 mg every 4 months Endometriosis: I.M.: Initial therapy may be with leuprolide alone or in combination with norethindrone; if retreatment for an additional 6 months is necessary, norethindrone should be used. Retreatment is not recommended for longer than one additional 6-month course. Lupron Depot®: 3.75 mg/month for up to 6 months or Lupron Depot-3®: 11.25 mg every 3 months for up to 2 doses (6 months total duration of treatment) Uterine leiomyomata (fibroids): I.M. (in combination with iron): Lupron Depot®: 3.75 mg/month for up to 3 months or Lupron Depot-3®: 11.25 mg as a single injection Administration Eligard®: Packaged in two syringes; one contains the Atrigel® polymer system, and the second contains leuprolide acetate powder; follow instructions for mixing; must be administered within 30 minutes of mixing. Lupron Depot®: Do not use needles smaller than 22 gauge; reconstitute only with diluent provided Viadur® implant: Requires surgical implantation and removal at 12-month intervals Implant (Viadur®): 65 mg [released over 12 months; packaged with administration kit] Supplied Injection, solution, as acetate (Lupron®): 5 mg/mL (2.8 mL) [contains benzyl alcohol; packaged with syringes and alcohol swabs] Injection, powder for reconstitution, as acetate [depot formulation; prefilled syringe]: Eligard®: 7.5 mg [released over 1 month] 22.5 mg [released over 3 months] 30 mg [released over 4 months] Lupron Depot®: 3.75 mg, 7.5 mg [released over 1 month; contains polysorbate 80] Lupron Depot®-3 Month: 11.25 mg, 22.5 mg [released over 3 months; contains polysorbate 80] Lupron Depot®-4 Month: 30 mg [released over 4 months; contains polysorbate 80] Lupron Depot-Ped®: 7.5 mg, 11.25 mg, 15 mg [released over 1 month; contains polysorbate 80] |
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octreotide (Sandostatin ® )
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Somatostatin analog. Dosing (Adults): Bleeding esophageal varices: IV bolus: 25-50 mcg followed by continuous IV infusion of 25-50 mcg/hour. Carcinoid tumors: Initial: 50 mcg IV/SQ qd-bid. Titrate dose based on response/tolerance. Range: 100-600 mcg/day in 2-4 divided doses - usual range 50-1500 mcg/day. VIPomas: Initial 2 weeks: 200-300 mcg/day IV/SQ in 2-4 divided doses. Titrate dose based on response/tolerance. Range: 150-750 mcg/day (doses >450 mcg/day are rarely required). Diarrhea: Initial: 50-100 mcg IV q8h - increase by 100 mcg/dose at 48-hour intervals. Maximum dose: 500 mcg q8h.
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vasopressin (Pitressin ® )
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ADH analog (Posterior pituitary hormone). Dosing (Adults): Diabetes insipidus: Note: Dosage is highly variable - titrated based on serum and urine sodium and osmolality in addition to fluid balance and urine output. 5-10 units IM/SQ 2-4 times daily as needed (dosage range 5-60 units/day). Abdominal distention: 5 units IM stat, then 10 units every 3-4 hours. GI hemorrhage: Continuous IV infusion: 0.5 milliunits/kg/hour (0.0005 unit/kg/hour). Double dosage as needed every 30 minutes to a maximum of 10 milliunits/kg/hour. IV: Initial: 0.2-0.4 unit/minute, then titrate dose as needed. If bleeding stops, continue at same dose for 12 hours, taper off over 24-48 hours. Out-of-hospital asystole (unlabeled use): Adults: 40 units IV. If spontaneous circulation is not restored in 3 minutes, then repeat dose. Pulseless VT/VF: 40 units IV (as a single dose only). If no IV access - administer 40 units diluted with NS (to a total volume of 10 ml) endotracheally. Vasodilatory shock/septic shock: Vasopressin may be used in patients with refractory shock despite adequate fluid resuscitation and the use of high-dose conventional catecholamines such as norepinephrine and dopamine, however, further studies are needed to determine its exact place in therapy. Current evidence does not support the use of vasopressin as a replacement for norepinephrine or dopamine as a first-line agent.
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any diagnosis or treatment made in reliance thereon. David F. McAuley, Pharm.D., R.Ph. GlobalRPh Inc. |
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