Gradient
Gradient Uses, Dosage, Side Effects, Food Interaction and all others data.
Gradient is the difluorinated derivative of cinnarizine. It is a seletive calcium channel antagonist and has H1-receptor blocking action. By reducing excessive transmembrane influx of calcium Gradient prevents cellular calcium overlod. It does not interfere with normal cellular calcium homeostasis. Gradient also has some antihistaminic and sedative properties.
Gradient is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity.
| Trade Name | Gradient |
| Generic | Flunarizine |
| Flunarizine Other Names | Flunarizina, Flunarizine, Flunarizinum |
| Type | |
| Formula | C26H26F2N2 |
| Weight | Average: 404.4948 Monoisotopic: 404.206405252 |
| Protein binding | 99% bound to plasma proteins |
| Groups | Approved |
| Therapeutic Class | Miscellaneous prophylactic migraine preparations |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Gradient is used for
- Prophylaxis of classic (with aura) or common (without aura) migraine
- Symptomatic treatment of vestibular vertigo (due to a diagnosed functional disorder of the vestibular system).
- Peripheral Vascular Disease (PVD)
- Motion sickness
- Refractory epilepsy resistant to conventional antiepileptic therapy.
Gradient is also used to associated treatment for these conditions: Severe Migraine
How Gradient works
Gradient inhibits the influx of extracellular calcium through myocardial and vascular membrane pores by physically plugging the channel. The decrease in intracellular calcium inhibits the contractile processes of smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.
Dosage
Gradient dosage
Migraine Prophylaxis:
- Starting Dose: 10 mg at night in patients less than 65 years of age and 5 mg daily in patients older than 65 years. If, during this treatment depressive, extrapyramidal or other unacceptable symptoms occur, administration should be discontinued. If, after 2 months of this initial treatment, no significant improvement is observed, the patient should be considered a non-responder and administration should be discontinued.
- Maintenance Treatment: If a patient is responding satisfactorily and if a maintenance treatment is needed, the dose should be decreased to 5 days treatment at the same daily dose with two successive medicine free days every week. Even if the prophylactic maintenance treatment is successful and well tolerated, it should be interrupted after 6 months and it should be re-initiated only if the patient relapses.
Peripheral Vascular disease: 10 mg twice daily, up to 30 mg per day if required.
Vertigo & motion sickness: 10-20 mg daily for adults and 5 mg daily for children (> 40 kg).
Epileptic seizure: 15-20 mg daily in adults and 5 to 10 mg daily for children as an add-on therapy
Side Effects
Gradient is well tolerated and seldom causes serious side effects. The main adverse effects experienced by the patients are as follows:
Central nervous system: Depression, drowsiness, sedation, and anxiety.
Gastrointestinal: Heart burn, nausea, emesis, dry mouth, gastralgia.
Miscellaneous: Weight gain, and/or increased appetite, asthenia, muscle aches, skin rash, and galactorrhea in female patients on oral contraceptives.
Toxicity
-Gradient should be used with care in patients with depression or those being prescribed other agents, such as phenothiazines, concurrently, which may cause extrapyramidal side-effects. -Acute overdosage has been reported and the observed symptoms were sedation, agitation and tachycardia. -Treatment of acute overdosage consists of charcoal administration, induction of emesis or gastric lavage, and supportive measures. No specific antidote is known.
Precaution
Since sedation or drowsiness occur in some patients during treatment with flunarizine hydrochloride, patients should be cautioned against activities which require alertness or rapid, precise responses (e.g. operating machinery or a motor vehicle) until the response to the drug has been determined.
Interaction
Galactorrhoea has been reported in few women on oral contraceptives within the first two months of Gradient treatment. Hepatic enzyme inducers such as Carbamazepine and Phenytoin may interact with flunarizine by increasing its metabolism. So an increase in dosage of flunarizine may be required.
Food Interaction
- Avoid alcohol.
- Take with or without food. The absorption is unaffected by food.
Elimination Route
85% following oral administration.
Half Life
18 days
Pregnancy & Breastfeeding use
Safety in pregnancy and lactation has not been established.
Contraindication
Hypersensitivity to Gradient. Gradient is contra-indicated in patients with a history of depressive illness, or with pre-existing symptoms of Parkinson's disease or other extrapyramidal disorders.
Storage Condition
Store at a cool & dry place, protected from light and moisture. Keep out of reach of the children.
Innovators Monograph
You find simplified version here Gradient
FAQ
What is Gradient used for?
Gradient is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity. It is effective in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an adjuvant in the therapy of epilepsy.
How safe is Gradient?
Gradient may be safe, effective, and well-tolerated as a prophylactic treatment for episodic migraine, according to a systematic review and pooled meta-analysis published in Pain.
How does Gradient work?
Gradient is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity. Gradient inhibits the influx of extracellular calcium through myocardial and vascular membrane pores by physically plugging the channel.
What are the common side effects of Gradient?
The common side effects of Gradient are tiredness, drowsiness, weight gain and low mood. Possible weight gain is caused by an increase in appetite and can be avoided by your child following his or her usual diet without any increase in portion size.
Is Gradient safe during pregnancy?
Gradient probably is compatible with pregnancy.
Is Gradient safe during breastfeeding?
No information is available on the use of Gradient during breastfeeding.
Can I drink alcohol with Gradient?
Alcohol may increase the risk of tiredness and drowsiness with Gradient. If you do feel tired or drowsy whilst taking Gradient, you should avoid alcoholic drinks.
Can I drive after taking Gradient?
Gradient may cause drowsiness. If affected, do not drive or take part in any activity in which you need to be alert or need to see clearly.
When should be taken of Gradient?
Gradient should be taken at night-time starting with a low dose. This may then be increased as recommended by the doctor. You should encourage your child to continue with the medicine as it may not take full effect for about eight to 12 weeks.
How often can I take Gradient?
The recommended adult dose of Gradient is 10 mg daily taken in the evening with or without food. Those who have side effects may find 5 mg daily in the evening to be effective.
How long does Gradient take to work?
It may take 6 to 8 weeks of continued treatment before the maximum effect of this Gradient is noted.
How long does Gradient take to work?
Gradient has a long elimination half-life of about 19 days.
How long does Gradient last?
Gradient will usually be used for at least six months but you will be advised further about this by your doctor.
Who should not take Gradient?
Gradient should not be taken by people with depression or by people with Parkinson's disease or movement disorders.
Can Gradient increase blood pressure?
Gradient is reported to produce only slight decreases of systemic arterial blood pressure.
Does Gradient cause depression?
In contrast, Gradient, a calcium-channel antagonist used for acute and prophylactic treatment of migraine headaches, has been associated with depression.
Can I just stop taking Gradient?
It is not advisable to stop using this product suddenly, particularly if you have been on it for several weeks. If you are considering stopping the medication, talk to your doctor or pharmacist first. It must be used regularly and continuously to maintain its beneficial effects.
What happen If I missed dose of Gradient?
If you miss a dose, take it as soon as remembered; do not take it if it is near the time for the next dose, instead, skip the missed dose and resume your usual dosing schedule. Do not double-up the dose to catch up.
What happens if I overdose?
Symptoms of overdose may include confusion, unusual drowsiness, and rapid pulse.
Can Gradient affects my heart ?
Gradient caused an increase in heart rate following the administration of the higher doses.
