A drug commonly used to treat hyperparathyroidism.
Sensipar or cinacalcet is used to treat increased amounts of parathyroid hormone in people with long-term kidney disease on dialysis.
It is also used to treat increased amounts of calcium in people with an overactive parathyroid gland or in people with cancer of the parathyroid gland.
Cinacalcet works by decreasing the amount of parathyroid hormone, calcium, and phosphorus in your body. Having the correct amount of these substances in your body helps prevent bone disease.
What conditions does sensipar treat?
- Increased calcium in the blood due to parathyroid cancer.
- Hyperparathyroidism is caused by chronic kidney failure on dialysis.
- High level of calcium in the blood due to hyperparathyroidism.
How to use the senior
Take this medication by mouth with food or shortly after food, as directed by your doctor.
The manufacturer orders not to divide the tablet before taking it. However, many similar medications (immediate-release tablets) can be split/crushed. Follow your doctor’s instructions on how to take this medicine.
It can cause nausea, vomiting, or unusual tiredness. Tell your doctor or pharmacist immediately if any of these effects persist or get worse.
Sensipar can cause low levels of calcium in the blood. Your doctor will monitor your blood calcium levels while taking this medicine. Tell your doctor right away if you have any of the following symptoms of low calcium levels:
- Severe muscle spasms
- Numbness or tingling of the skin.
- Unusual tiredness
- Very fast/irregular/pounding heartbeat.
Tell your doctor right away if you have any severe side effects, including:
- Black or bloody stools.
- Stomach or abdominal pain
- Vomiting that contains blood or looks like coffee grounds.
Allergic reactions to the medicine are unusual. If you notice any of these symptoms while consuming the drug, seek medical help as urgently as possible:
- Swelling or itching (specifically in the throat, tongue, or face).
- Severe dizziness
- Difficulty breathing.
Uses in pregnancy and lactation
Limited case reports of use in pregnant women are insufficient to report a drug-associated risk of adverse developmental outcomes.
In animal reproduction studies, when female rats were exposed to the drug during the period of organogenesis until weaning at 2-3 times the systemic levels of the drug (based on AUC) at the maximum recommended human dose (MRHD) of 180 mg/day, peripartum.
A premature loss of postnatal puppies and a reduced body weight gain of puppies were observed in the presence of maternal hypocalcemia.
There are no data regarding the presence in human milk or the effects on the infant or milk production; studies in rats showed that cinacalcet was excreted in the milk; the developmental and health benefits of breastfeeding should be considered in conjunction with the mother’s clinical need for therapy and any potential adverse effects on the nursing infant from the treatment or an underlying maternal condition.
Interactions with other medications can change how your drugs work or increase the risk of severe side effects.
Severe – use the alternative
- Erythromycin base.
- Erythromycin ethylsuccinate.
- Erythromycin lactobionate.
- Erythromycin stearate.
- Grass of San Juan.
- DHEA, herbs.
- Eslicarbazepine acetate.
Mechanism of action
It increases the sensitivity of the Ca sensing receptor in parathyroid cells to activation by extracellular Ca, which negatively regulates PTH levels and consequently decreases serum Ca and phosphorus.
Bioavailability: high-fat food increases peak plasma concentration and AUC relative to fasting.
Peak plasma time: 2-6 h.
Limited protein: 93-97%.
Vd: 1000 L.
Metabolism: metabolized by CYP3A4, CYP2D6, and CYP1A2.
Metabolites: hydrocinnamic and hydroxy-hydrocinnamic acid, molecules containing naphthalene rings, dihydrodiols.
Inhibited enzyme: CYP2D6.
Excretion: Urine (80%); feces (15%).
- It should not be started in severe hypocalcemia (serum Ca <lower limit of normal).
Seizures (mainly generalized or tonic-clonic) were observed in clinical trials (1.4% compared to 0.7% in placebo).
It is not for the therapy of patients with chronic kidney disease who are not on dialysis due to an increased risk of hypokalemia.
Exposure to Cinacalcet is increased in patients with moderate and severe hepatic impairment; closely monitor serum calcium, serum phosphorus, and intact parathyroid hormone.
In cases of gastrointestinal bleeding, mostly upper gastrointestinal bleeding, reported in patients using calcimimetics, the exact cause of gastrointestinal bleeding is unknown.
Patients with risk factors for upper gastrointestinal bleeding (such as gastritis, esophagitis, ulcers, or severe vomiting) may be at increased risk of gastrointestinal bleeding when receiving treatment.
Monitor patients for worsening of common gastrointestinal adverse reactions of nausea and vomiting associated with therapy and for signs and symptoms of gastrointestinal bleeding and ulcerations during therapy; promptly evaluate and treat any suspicious gastrointestinal bleeding.
Adynamic bone disease can develop if PTH levels are <100 pg/ml.