Conivaptan

Generic name: conivaptan
Brand name: Vaprisol
Dosage form: intravenous solution (20 mg/100 mL-D5%)
Drug class: Vasopressin antagonists

Medically reviewed by  A Ras MD.

What is conivaptan?

Conivaptan is a prescription medicine that is used to treat low sodium levels.

Description

Conivaptan hydrochloride is chemically [1,1′-biphenyl]-2-carboxamide, N-[4-[(4,5-dihydro-2-methylimidazo[4,5-d][1]benzazepin-6(1H)-yl)carbonyl]phenyl]-, monohydrochloride, having a molecular weight of 535.04 and molecular formula C32H26N4O2∙HCl. The structural formula of conivaptan hydrochloride is:

Structural Formula

Conivaptan hydrochloride is a white to off-white or pale orange-white powder that is very slightly soluble in water (0.15 mg/mL at 23° C). Conivaptan hydrochloride injection is supplied as a sterile premixed solution with dextrose in a flexible plastic container.

Each container contains a clear, colorless, sterile, non-pyrogenic solution of conivaptan hydrochloride in dextrose injection for intravenous use. Each 100 mL, single-use premixed INTRAVIA Container contains 20 mg of conivaptan hydrochloride and 5 g of Dextrose Hydrous, USP. Lactic Acid, USP is added for pH adjustment to pH 3.4 to 3.8. The flexible plastic container is fabricated from a specially designed multilayer plastic (PL 2408).

Solutions in contact with the plastic container leach out certain of the chemical components from the plastic in very small amounts; however, biological testing was supportive of the safety of the plastic container materials. The flexible container has a foil overwrap. Water can permeate the plastic into the overwrap, but the amount is insufficient to affect the premixed solution significantly.

Mechanism of Action

Conivaptan hydrochloride is a dual arginine vasopressin (AVP) antagonist with nanomolar affinity for human V1A and V2 receptors in vitro. The level of AVP in circulating blood is critical for the regulation of water and electrolyte balance and is usually elevated in both euvolemic and hypervolemic hyponatremia. The AVP effect is mediated through V2 receptors, which are functionally coupled to aquaporin channels in the apical membrane of the collecting ducts of the kidney.

These receptors help to maintain plasma osmolality within the normal range. The predominant pharmacodynamic effect of conivaptan hydrochloride in the treatment of hyponatremia is through its V2 antagonism of AVP in the renal collecting ducts, an effect that results in aquaresis, or excretion of free water.

Before taking conivaptan, tell your doctor:

  • If you are allergic to conivaptan; any part of this medicine; or any other drugs, foods, or substances. Tell your doctor about the allergy and what signs you had.
  • If you are not able to pass urine.
  • If you have kidney disease.
  • If you have low blood volume.
  • If you take any drugs (prescription or OTC, natural products, vitamins) that must not be taken with conivaptan, like certain drugs that are used for HIV, infections, or depression. There are many drugs that must not be taken with conivaptan. Your doctor or pharmacist can tell you if you are taking a drug that must not be taken with conivaptan.
  • If you are breast-feeding. Do not breast-feed while you take conivaptan.

This is not a list of all drugs or health problems that interact with conivaptan.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take conivaptan with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

What are some things I need to know or do while I take conivaptan?

  • Tell all of your health care providers that you take conivaptan. This includes your doctors, nurses, pharmacists, and dentists.
  • To lower the chance of feeling dizzy or passing out, rise slowly if you have been sitting or lying down. Be careful going up and down stairs.
  • Have blood work checked as you have been told by the doctor. Talk with the doctor.
  • Very bad and sometimes deadly effects may happen from fixing low sodium levels too fast. The chance is raised in people with poor nutrition, very bad liver disease, or alcohol addiction. Talk with your doctor.
  • This medicine may cause fertility problems. This may affect being able to have children. Talk with the doctor.
  • Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using conivaptan while you are pregnant.

How is conivaptan best taken?

Use conivaptan as ordered by your doctor. Read all information given to you. Follow all instructions closely.

  • It is given as an infusion into a vein over a period of time.

What do I do if I miss a dose?

  • Call your doctor to find out what to do.

What are the side effects of conivaptan that I need to call my doctor about immediately?

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

  • Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
  • Signs of fluid and electrolyte problems like mood changes, confusion, muscle pain or weakness, a heartbeat that does not feel normal, very bad dizziness or passing out, fast heartbeat, more thirst, seizures, feeling very tired or weak, not hungry, unable to pass urine or change in the amount of urine produced, dry mouth, dry eyes, or very bad upset stomach or throwing up.
  • Signs of a urinary tract infection (UTI) like blood in the urine, burning or pain when passing urine, feeling the need to pass urine often or right away, fever, lower stomach pain, or pelvic pain.
  • Signs of high or low blood pressure like very bad headache or dizziness, passing out, or change in eyesight.
  • Trouble swallowing or speaking.
  • Swelling in the arms or legs.
  • This medicine may cause tissue damage if the drug leaks from the vein. Tell your nurse if you have any redness, burning, pain, swelling, blisters, skin sores, or leaking of fluid where the drug is going into your body.

What are some other side effects of conivaptan?

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

  • Irritation where conivaptan is used.
  • Headache.
  • More thirst.
  • Diarrhea or constipation.
  • Upset stomach or throwing up.
  • Trouble sleeping.
  • Throat pain.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-332-1088. You may also report side effects at https://www.fda.gov/medwatch.

If overdose is suspected:

If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

How do I store and/or throw out conivaptan?

  • If you need to store conivaptan at home, talk with your doctor, nurse, or pharmacist about how to store it.
SRC: NLM .