Acrivastine – Overview

What is Acrivastine?

Acrivastine is a triprolidine analog antihistamine indicated for the treatment of allergies and hay fever. As an H1 receptor antagonist, it functions by blocking the action of histamine at this receptor thereby preventing the symptoms associated with histamine release such as pruritis, vasodilation, hypotension, edema, bronchoconstriction, and tachycardia. Acrivastine is currently available in combination with pseudoephedrine as the FDA-approved product Semprex-D.

Acrivastine capsule.jpg

Brand Names

Semprex-D, Benadryl®

What is the proper storage of Acrivastine?

  • Keep all medicines out of the reach and sight of children.
  • Store in a cool, dry place, away from direct heat and light

Identity of Acrivastine

Type of medicine Antihistamines
Synonyms Acrivastina, Acrivastine
Molecular Formula C22H24N2O2
Molecular Weight 348.438 g/mol
IUPAC Names (E)-3-{6-[(E)-1-(4-methylphenyl)-3-pyrrolidin-1-yl- prop-1-enyl]pyridin-2-yl}prop-2-enoic acid
Structural formula of main components Acrivastine structure.png
Pure active ingredient Acrivastine
Appearance White to pale cream crystalline powder
Melting point 222°C
Available as Capsules
Prescription Acrivastine is available on prescription

What is Acrivastine used for?

Acrivastine is used in the treatment of:

  • Allergic Rhinitis
  • Nasal Congestion

What side effects may I notice from receiving Acrivastine?

Side effects that you should report to your doctor or health care professional as soon as possible:

  • Allergic reactions like skin rash or hives, swelling of the face, lips, or tongue
  • Breathing problems
  • Changes in vision
  • Dizziness
  • Eye pain
  • Fast, irregular heartbeat
  • High blood pressure
  • Nervousness
  • Restlessness
  • Seizures
  • Tremor
  • Trouble passing urine or change in the amount of urine
  • Trouble sleeping
  • Unusually weak or tired

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):

  • Drowsiness
  • Dry mouth
  • Headache
  • Loss of appetite
  • Nausea
  • Sore throat
  • Stomach upset
  • Tiredness

This list may not describe all possible side effects. Call your doctor for medical advice about side effects.

How does Acrivastine work?

Benadryl allergy relief capsules contain the active ingredient acrivastine, which is a type of medicine called a non-sedating antihistamine. What other drugs will affect amlodipine?

Acrivastine works by preventing the actions of histamine – a substance produced by the body when it reacts to a foreign substance, such as pollen or pet fur (these are known as allergens). Histamine causes a chain reaction that results in allergic symptoms such as itchy eyes, sneezing and a runny nose. Acrivastine blocks histamine receptors and so stops this chain reaction.

Acrivastine can also be used to relieve the symptoms of a condition called chronic idiopathic urticaria. This is a chronic itchy rash, similar to nettle rash, but with no apparent cause. Blocking the actions of histamine relieves the itching and reduces the rash associated with this condition and other allergic skin reactions.

Acrivastine starts working in about 15 minutes and should provide relief from hay fever symptoms within an hour of taking a dose.

What may interact with this medication?

Do not take this medicine with any of the following medications:

  • Antihistamines and other medicines for allergy, cough and cold
  • Ergot alkaloids like dihydroergotamine, ergonovine, ergotamine, methylergonovine
  • Herbal or dietary supplements containing ephedra or ephedrine
  • MAOIs like Carbex, Eldepryl, Marplan, Nardil, and Parnate

This medicine may also interact with the following medications:

  • Alcohol
  • Certain medicines for depression
  • Linezolid
  • Medicines for anxiety or sleep
  • Medicines for blood pressure
  • Narcotic medicines for pain
  • Procarbazine
  • Stimulant medicines for attention disorders, weight loss, or to stay awake
  • Yohimbine

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

Dosage and Administration

The recommended dosage for adults and adolescents 12 years and older is one capsule administered orally, every 4 to 6 hours four times a day.

Overdose

There have been no reports of overdosage with Semprex-D Capsules. In the clinical trial program and in international post-marketing experience, there have been two reported overdoses with acrivastine. Doses were 72 mg and 322 mg. Both patients recovered without sequelae. Adverse events included trembling, stridor, loss of consciousness and possible convulsions in the first patient and somnolence in the second.

Since acrivastine and pseudoephedrine have pharmacologically different actions, it is difficult to predict how an individual will respond to overdosage with SEMPREX-D Capsules. However, acute overdosage with SEMPREX-D Capsules may produce clinical signs of either CNS stimulation or depression. Overdosage of sympathomimetics has been associated with the following events: fear, anxiety, tenseness, restlessness, tremor, weakness, pallor, respiratory difficulty, dysuria, insomnia, hallucinations, convulsions, CNS depression, arrhythmias, and cardiovascular collapse with hypotension. Treatment for overdosage with SEMPREX-D Capsules should follow general symptomatic and supportive principles.

Precautions

It is very important that your doctor check your progress at regular visits. This will allow you to see if the medicine is working properly and to decide if you should continue to take it.

Do not use this medicine and an MAO inhibitor (MAOI) such as Eldepryl®, Marplan®, Nardil®, or Parnate® within 14 days of each other.

This medicine may cause some people to become dizzy, drowsy, or less alert than they are normally. Make sure you know how you react to this medicine before you drive, use machines, or do anything else that could be dangerous if you are dizzy or are not alert.

This medicine will add to the effects of alcohol and other CNS depressants (medicines that make you drowsy or less alert). Some examples of CNS depressants are antihistamines or medicine for hay fever, other allergies, or colds, sedatives, tranquilizers, or sleeping medicine, prescription pain medicine or narcotics, barbiturates, medicine for seizures, muscle relaxants, or anesthetics, including some dental anesthetics. Check with your medical doctor or dentist before taking any of the above while you are taking this medicine.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.

Acrivastine and pregnancy

Acrivastine is not usually recommended during pregnancy because there is very little information about its use in pregnancy. Other antihistamines that we know more about may be more suitable.

If you think you need to take acrivastine in pregnancy, talk to your doctor or pharmacist. They will be able to help you decide, or may suggest other medicines for you.

Acrivastine and breastfeeding

If your doctor or health visitor says your baby is healthy, you can use acrivastine while breastfeeding, but it is better to take occasional doses or only for a short time.

We do not know how much acrivastine gets into breast milk, so it is better to take an antihistamine which we know more about.

If you’re breastfeeding, or planning to breastfeed, talk to your doctor. They may prescribe similar antihistamines, called loratadine or cetirizine, that are more suitable while you’re breastfeeding.

Talk to your doctor, pharmacist, midwife or health visitor if your baby is not feeding as well as usual, seems unusually sleepy, seems irritable, or if you have any other concerns about your baby.

Acrivastine and fertility

There’s no evidence to suggest that taking acrivastine will reduce fertility in either men or women. But speak to a pharmacist or your doctor before taking it if you’re trying to get pregnant.

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