Cinacalcet Hydrochloride Tablets 60mg

Cinacalcet Hydrochloride Tablets 30mg
Cinacalcet Hydrochloride Tablets 60mg
Cinacalcet Hydrochloride Tablets 90mg

DESCRIPTION

Cinacalcet is used to treat hyperparathyroidism in patients with chronic kidney disease who are on dialysis. Hyperparathyroidism is a condition that is caused when the parathyroid glands located in the neck make too much parathyroid hormone (PTH). This hormone helps to control the concentrations of calcium and phosphorus in your blood.

Cinacalcet lowers the amount of PTH which lowers the calcium and phosphorus concentrations. Cinacalcet is also used to lower calcium in the blood of patients with parathyroid cancer and primary hyperparathyroidism.

This medicine is available only with your doctor’s prescription.

COMPOSITION

a) Cinacalcet hydrochloride 30mg Taj Pharma:

Each tablet contains:

Cinacalcet hydrochloride equivalent to cinacalcet 30mg
Excipients q.s

b) Cinacalcet hydrochloride 60mg Taj Pharma:

Each tablet contains:

Cinacalcet hydrochloride equivalent to cinacalcet 60mg
Excipients q.s

c) Cinacalcet hydrochloride 90mg Taj Pharma:

Each tablet contains:

Cinacalcet hydrochloride equivalent to cinacalcet 90mg
Excipients q.s.

USES

Cinacalcet is used to treat increased amounts of a certain hormone (parathyroid) in people with long-term kidney disease who are 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 right amount of these substances in your body helps to prevent bone disease.

PHARMACOLOGY

Mechanism of Action

Increases sensitivity of Ca-sensing receptor in parathyroid cells to activation by extracellular Ca, thereby downregulating PTH levels and consequently lowering serum Ca & phosphorus

Absorption

Bioavailability: High-fat meal increases both peak plasma concentration and AUC vis-a-vis fasting

Peak Plasma Time: 2-6 hr

Distribution

Protein Bound: 93-97%

Vd: 1000 L

Metabolism

Metabolism: metabolized by CYP3A4, CYP2D6 & CYP1A2

Metabolites: hydrocinnamic and hydroxy-hydrocinnamic acid, naphthalene-ring-containing molecules, dihydrodiols

Enzyme Inhibited: CYP2D6

Elimination

Half-Life: 30-40 hr

Excretion: Urine (80%); feces (15%)

Dosage Forms & Strengths

tablet

30mg
60mg
90mg

Primary Hyperparathyroidism (HPT)

Indicated for severe hypercalcemia in patients who are unable to undergo parathyroidectomy

Initial dose: 30 mg PO q12hr

May increase if needed at 2-4 week intervals through sequential doses 60 mg q12hr, 90 mg q12hr, or 90 mg q6-8hr as necessary to normalize serum calcium levels

Secondary Hyperparathyroidism

Indicated in patients with chronic kidney disease (CKD) on dialysis

Initial dose: 30 mg PO day

May increase if needed by titrating at 2-4 week intervals through sequential doses of 60, 90, 120, or 180 mg day

Parathyroid Carcinoma

Indicated to treat hypercalcemia in patients with parathyroid carcinoma

Initial dose: 30 mg PO q12hr

May increase if needed at 2-4 week intervals through sequential doses 60 mg q12hr, 90 mg q12hr, or 90 mg q6-8hr as necessary to normalize serum calcium levels

Renal Impairment

Dose adjustment not necessary

Hepatic Impairment

Moderate to severe hepatic impairment: Monitor serum calcium, serum phosphorus, and iPTH levels throughout treatment

ADMINISTRATION

Oral Administration

Take with food or shortly after a meal

Swallow tablet whole, do not chew, crush, or divide

Dosing Considerations

Monitor for hypocalcemia once maintenance dose established

Parathyroid carcinoma or primary hyperparathyroidism

Monitor serum calcium every 2 months

Hyperparathyroidism in patients with CKD on dialysis

Monitor serum calcium monthly
For calcium levels between 7.5-8.4 mg/dL or if hypocalcemia symptoms occur, may administer calcium-containing phosphate binders and/or vitamin D sterols to raise serum calcium
If calcium levels <7.5 mg/dL or hypocalcemia symptoms persist and the dose of vitamin D cannot be increased, withhold therapy until calcium levels reach 8 mg/dL and/or hypocalcemia symptom resolve, then reinitiate using next lowest dose

PREGNANCY & LACTATION

Pregnancy

Limited case reports of use in pregnant women are insufficient to inform 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 through to weaning at 2-3 times systemic drug levels (based on AUC) at maximum recommended human dose (MRHD) of 180 mg/day, peripartum and early postnatal pup loss and reduced pup body weight gain were observed in the presence of maternal hypocalcemia

Lactation

There are no data regarding presence in human milk or effects on breastfed infant or on milk production; studies in rats showed that cinacalcet was excreted in milk; developmental and health benefits of breastfeeding should be considered along with mother?s clinical need for therapy and any potential adverse effects on breastfed infant from therapy or from underlying maternal condition

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: Maybe acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

HOW TO USE:

Take this medication by mouth with food or shortly after a meal, as directed by your doctor. The manufacturer directs not to split the tablet before taking it. However, many similar drugs (immediate-release tablets) can be split/crushed. Follow your doctor’s directions on how to take this medication. The dosage is based on your medical condition, response to treatment, and laboratory tests. Take this medication regularly in order to get the most benefit from it. Remember to take it at the same time(s) each day.

WARNINGS

Contraindications

Hypersensitivity

Should not be initiated in severe hypocalcemia (serum Ca<=”” p=”” style=”box-sizing: border-box;”>

Cautions

History of seizure; seizures (primarily generalized or tonic-clonic) were observed in clinical trials (1.4% compared with 0.7% in placebo)

Not for therapy of patients with chronic kidney disease not on dialysis due to increased risk for hypokalemia

Drug exposure is increased in patients with moderate and severe hepatic impairment; monitor serum calcium, serum phosphorus, and intact parathyroid hormone closely

The adynamic bone disease may develop if PTH levels <100 pg/mL

Therapy is not indicated for patients with CKD, not on dialysis; long-term safety and efficacy of therapy not established in patients with secondary HPT and CKD, not on dialysis

Idiosyncratic cases of hypotension, worsening heart failure, and/or arrhythmia reported in patients with impaired cardiac function, in which a causal relationship to therapy could not be completely excluded and which may be mediated by reductions in serum calcium levels

Significant lowering of calcium by therapy can cause paresthesias, myalgias, muscle spasms, tetany, and seizures; life-threatening events and fatal outcomes associated with hypocalcemia reported in patients receiving treatment, including in pediatric patients

Gastrointestinal bleeding

Cases of gastrointestinal bleeding, mostly upper gastrointestinal bleeding, reported in patients using calcimimetics
The exact cause of GI bleeding is unknown; patients with risk factors for upper GI bleeding (such as known gastritis, esophagitis, ulcers or severe vomiting) may be at increased risk for GI bleeding when receiving treatment
Monitor patients for worsening of common GI adverse reactions of nausea and vomiting associated with therapy and for signs and symptoms of GI bleeding and ulcerations during therapy
Promptly evaluate and treat any suspected GI bleeding

QT interval prolongation and ventricular arrhythmia

Decreases in serum calcium can prolong the QT interval, potentially resulting in ventricular arrhythmia; cases of QT prolongation and ventricular arrhythmia reported in patients receiving therapy; patients with congenital long QT syndrome
History of QT interval prolongation, family history of long QT syndrome or sudden cardiac death, and other conditions that predispose to QT interval prolongation and ventricular arrhythmia may increase the risk for QT interval prolongation and ventricular arrhythmias
In patients at risk, receiving therapy, who develop hypocalcemia, closely monitor corrected serum calcium and QT interval

CONTRAINDICATIONS

Contraindicated

eliglustat
etelcalcetide

Serious – Use Alternative

carbamazepine
cimetidine
clarithromycin
dacomitinib
erythromycin base
erythromycin ethylsuccinate
erythromycin lactobionate
erythromycin stearate
ketoconazole
nefazodone
rifabutin
rifampin
St John’s Wort

Monitor Closely

abiraterone
amobarbital
aprepitant
armodafinil
artemether/lumefantrine
atazanavir
bosentan
aripiprazole
budesonide
bupropion
butabarbital
butalbital
codeine
conivaptan
cortisone
crizotinib
cyclosporine
darifenacin
darunavir
dasatinib
deferasirox
delavirdine
deutetrabenazine
dexamethasone
DHEA, herbal
diltiazem
dronedarone
efavirenz
eliglustat
eluxadoline
elvitegravir/cobicistat/emtricitabine/tenofovir DF
eslicarbazepine acetate
ethotoin
etravirine
eucalyptus
fedratinib
fluconazole
fludrocortisone
fluvoxamine
fosamprenavir
fosphenytoin
grapefruit
griseofulvin
hydrocortisone
indinavir
isoniazid
itraconazole
lapatinib
Retrovir
lofexidine
lorcaserin
lumefantrine
marijuana
methylprednisolone
metronidazole
miconazole vaginal
mirabegron
modafinil
nelfinavir
nevirapine
nifedipine
nilotinib
oxcarbazepine
oxiconazole
pentobarbital
phenobarbital
phenytoin
Proliant
posaconazole
prednisolone
prednisone
primidone
quinupristin/dalfopristin
rifapentine
ritonavir
rolapitant
rufinamide
secobarbital
tamoxifen
tamsulosin
topiramate
valentine
verapamil
voriconazole
vortioxetine
zafirlukast

SIDE EFFECTS

Nausea, vomiting, or unusual tiredness may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly. Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects. Cinacalcet can cause low calcium blood levels. Your doctor will check your calcium blood levels while you are taking this medication. Tell your doctor right away if you have any of the following symptoms of low calcium levels: numb/tingling skin, severe muscle spasms, seizures, fast/irregular/pounding heartbeat. Tell your doctor right away if you have any serious side effects, including black/bloody stools, stomach/abdominal pain, vomit that contains blood or looks like coffee grounds. A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing. This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

DRUG INTERACTIONS
Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor’s approval. If your doctor tells you to switch from using this medication to etelcalcetide, this medication should be stopped at least 7 days before starting etelcalcetide. Using both medications together may increase the risk of side effects (especially low calcium levels).

OVERDOSE

If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control centre right away. US residents can call their local poison control centre at 1-800-222-1222. Canada residents can call a provincial poison control centre. Symptoms of overdose may include severe muscle spasms, seizures.

ADVERSE EFFECTS

>10%

Secondary Parathyroidism

Diarrhoea (20%)
Nausea (19%)
Vomiting (15%)
Myalgia (14%)

1-10%

Secondary Parathyroidism

Dizziness (8%)
Hypertension (5%)
Access infection (4%)
Anorexia (4%)
Asthenia (4%)
Noncardiac chest pain (4%)
Seizures 1.4%

Frequency Not Defined

Parathyroid CA

Nausea/vomiting
Hypocalcemia

Postmarketing Reports

Hypotension

Worsening heart failure and/or arrhythmias

Adynamic bone disease

Gastrointestinal bleeding

Chondrocalcinosis pyrophosphate (acute pseudogout)

NOTES:

Do not share this medication with others. Laboratory and/or medical tests (such as calcium, phosphorus, parathyroid hormone levels) should be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.

MISSED DOSE:
If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

STORAGE:
Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets. Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

IMPORTANT: HOW TO USE THIS INFORMATION:

This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

Manufactured in India by:
TAJ LIFE SCIENCES PVT. LTD.
Unit No. 214, Old Bake House,
Bake House Lane, Fort,
Mumbai-400001
at: Ahmedabad- Gujarat, INDIA.
Ho.NO.+91 8448 444 095
Toll Free Phone: (1800-222-434 / 1800-222-825)