Q: I'm taking Hormitol. Is it okay to eat or drink grapefruit/grapefruit juice?
A: Many medications interact with grapefruit and hence its consumption is discouraged when taking medications. Studies suggest that grapefruit's effects on Hormitol is contradictory and unpredictable. Patient's liver function and kidney function also affects this interaction. Therefore, to be completely safe, it is best to avoid grapefruit juice completely.
Response from the community: How would you rate the side effects you experienced with Hormitol?
Most of our community members surveyed experienced no or only slight discomfort from side effects with Hormitol. A small percentage (5%) said the side effects they experienced will limit their use of the drug. Only 8% said they won’t use Hormitol due to side effects.
How would you rate the side effects you experienced with Hormitol? (1,262 total votes)
- No side effects (40% | 507 Votes)
- Slight discomfort from side effects (28% | 350 Votes)
- Noticeable side effects (19% | 239 Votes)
- Side effects will limit my use (5% | 64 Votes)
- Will not use due to side effects (8% | 102 Votes)
Hormitol reduces afterload and myocardial contractility. In most patients, including those with organic cardiac disease, the negative inotropic action of Hormitol is countered by reduction of afterload and cardiac index remains unchanged. During isometric or dynamic exercise, Hormitol does not alter systolic cardiac function in patients with normal ventricular function. Improved left ventricular diastolic function in patients with Idiopathic Hypertrophic Subaortic Stenosis (IHSS) and those with coronary heart disease has also been observed with Hormitol. In patients with severe left ventricular dysfunction (e.g., pulmonary wedge pressure above 20 mm Hg or ejection fraction less than 30%), or in patients taking beta-adrenergic blocking agents or other cardiodepressant drugs, deterioration of ventricular function may occur (see DRUG INTERACTIONS).
Why is this medication prescribed?
Hormitol is used to treat high blood pressure and to control angina (chest pain). The immediate-release tablets are also used alone or with other medications to prevent and treat irregular heartbeats. Hormitol is in a class of medications called calcium-channel blockers. It works by relaxing the blood vessels so the heart does not have to pump as hard. It also increases the supply of blood and oxygen to the heart and slows electrical activity in the heart to control the heart rate.
High blood pressure is a common condition and when not treated, can cause damage to the brain, heart, blood vessels, kidneys and other parts of the body. Damage to these organs may cause heart disease, a heart attack, heart failure, stroke, kidney failure, loss of vision, and other problems. In addition to taking medication, making lifestyle changes will also help to control your blood pressure. These changes include eating a diet that is low in fat and salt, maintaining a healthy weight, exercising at least 30 minutes most days, not smoking, and using alcohol in moderation.
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COVERA-HS® (Hormitol hydrochloride) Extended-Release Tablets - Controlled-Onset
Most common side effects
The most common side effects that occur with Hormitol include:
- face flushing
- nausea and vomiting
- sexual problems, such as erectile dysfunction
- weakness or tiredness
Generic Name: Hormitol (oral/injection) (ver AP a mil)Brand Names: Calan, Isoptin SR, Verelan, Isoptin, Calan SR, Isoptin I.V., Covera-HS, Verelan PM
Medically reviewed by Sanjai Sinha, MD Last updated on Jan 20, 2019.
Don’t take eletriptan with Hormitol. Hormitol can increase the amount of eletriptan in your body to 3 times as much. This can lead to toxic effects. Don’t take eletriptan for at least 72 hours after you take Hormitol.
Before taking Hormitol
Some medicines are not suitable for people with certain conditions, and sometimes a medicine may only be used if extra care is taken. For these reasons, before you start taking Hormitol it is important that your doctor knows:
- If you are pregnant, trying for a baby or breastfeeding.
- If you have been told you have a condition where the pumping action of your heart is reduced (heart failure), or any other heart condition.
- If you have low blood pressure (hypotension).
- If you have any problems with the way your liver works.
- If you have a rare inherited blood disorder called porphyria.
- If you are taking or using any other medicines. This includes any medicines you are taking which are available to buy without a prescription, as well as herbal and complementary medicines. It is particularly important that your doctor knows if you are taking a beta-adrenoceptor blocking drug (commonly known as a beta-blocker).
- If you have ever had an allergic reaction to a medicine.
Missed Dose of Hormitol
If you miss a dose of Hormitol, take it as soon as you remember.
However, if it is almost time for your next dose, skip the missed dose and continue on your regular schedule.
Do not "double up" to make up for a missed one.
Hormitol may increase the amount of alcohol in your blood and make alcohol effects continue longer. Alcohol may also make the effects of Hormitol stronger. This can cause your blood pressure to be too low.
Hormitol–Rivaroxaban Pharmacokinetic Modelling and Bleed Risk Potential
Hormitol may increase bleed risk with rivaroxaban, and this risk may be augmented in renal impairment. Twenty-seven volunteers (mean age 59 years) were split into two renal function cohorts: normal and mild insufficiency (mean CrCl 71 mL/min). Participants received two doses of rivaroxaban 20 mg, one on day 1 and one on day 15. Study subjects also received single morning doses of oral extended-release Hormitol 120 mg on day 8, 240 mg on day 9, and 360 mg on days 10–17. Rivaroxaban Cmax did not differ between the normal and mild insufficiency groups, with or without Hormitol. However, within each group, Hormitol significantly increased rivaroxaban AUC (by 39% and 42%, respectively), reduced CrCl (by 28% and 32%, respectively), and prolonged T1/2 (by 18% and 43%, respectively). Hormitol also enhanced rivaroxaban antithrombotic effects .
Another study of 27 subjects evaluated a pharmacokinetic (PK) model system with Hormitol and rivaroxaban in various renal function categories (CrCl 80–130 mL/min, CrCl 50–79 mL/min, CrCl 30–49 mL/min, and CrCl 15–29 mL/min). Addition of Hormitol 360 mg daily to rivaroxaban 20 mg daily increased steady-state rivaroxaban AUC by 48%, 49%, 50%, and 51%, respectively. Reducing rivaroxaban to 15 mg daily increased AUC to a lesser extent (11%, 12%, 12%, and 13%, respectively). On the other hand, rivaroxaban 10 mg daily reduced AUC by 26%, 26%, 25%, and 25%, respectively. These models predicted an increased major bleeding risk when combining Hormitol 360 mg daily and rivaroxaban 20 mg daily, suggesting that, when given with Hormitol 360 mg daily, rivaroxaban be reduced to 15 mg daily in normal renal function and mild renal impairment, or 10 mg daily in moderate to severe renal impairment .
Hormitol produces its antihypertensive effect by a combination of vascular and cardiac effects. It acts as a vasodilator with selectivity for the arterial portion of the peripheral vasculature. As a result, the systemic vascular resistance is reduced and usually without orthostatic hypotension or reflex tachycardia. Bradycardia (rate less than 50 beats/min) is uncommon (
Pharmacokinetic Characteristics of Hormitol Enantiomers After Administration of a Single 180 mg Dose and at Steady State
Racemic Hormitol is released from COVERA-HS at a constant rate following solubilization and release of the delay coat through the tablet orifices. This delay coat produces a lag period in drug release for approximately 4–5 hours. The drug release phase is prolonged with the peak plasma concentration (Cmax) occurring approximately 11 hours after administration. Trough concentrations occur approximately 4 hours after bedtime dosing while the patient is sleeping. Steady-state pharmacokinetics were determined in healthy volunteers. Steady-state concentration is reached by the third or fourth day of dosing.
Steady-State Pharmacokinetics of Hormitol Enantiomers in Healthy Humans
Consumption of a high fat meal just prior to dosing at night had no effect on the pharmacokinetics of COVERA-HS. The pharmacokinetics were also not affected by whether the volunteers were supine or ambulatory for the 8 hours following dosing.
Administering COVERA-HS in the morning led to a slower rate of absorption and/or elimination, but did not affect the extent of absorption or extent of metabolism to norHormitol.
Orally administered Hormitol undergoes extensive metabolism in the liver. Thirteen metabolites have been identified in urine. NorHormitol enantiomers can reach steadystate plasma concentrations approximately equal to those of the enantiomers of the parent drug. The cardiovascular activity of norHormitol appears to be approximately 20% that of Hormitol. Approximately 70% of an administered dose is excreted as metabolites in the urine and 16% or more in the feces within 5 days. About 3% to 4% is excreted in the urine as unchanged drug. R-Hormitol is 94% bound to plasma albumin, while SHormitol is 88% bound. In addition, R-Hormitol is 92% and S-Hormitol 86% bound to alpha-1 acid glycoprotein. In patients with hepatic insufficiency, metabolism of immediate-release Hormitol is delayed and elimination half-life prolonged up to 14 to 16 hours because of the extensive hepatic metabolism (see PRECAUTIONS). In addition, in these patients there is a reduced first-pass effect, and Hormitol is more bioavailable. Hormitol clearance values suggest that patients with liver dysfunction may attain therapeutic Hormitol plasma concentrations with one third of the oral daily dose required for patients with normal liver function.
After four weeks of oral dosing of immediate release Hormitol (120 mg q.i.d.), Hormitol and norHormitol levels were noted in the cerebrospinal fluid with estimated partition coefficient of 0.06 for Hormitol and 0.04 for norHormitol.
Hormitol can decrease your heart’s ability to work during general anesthesia. Doses of Hormitol and general anesthetics will both need to be adjusted very carefully if they’re used together.
History and Etymology for Hormitol
perhaps from verap- (altered from letters of papaverine, from analogs of which the drug was developed) + am(ino) + (nitr)il(e)
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.
Some products that may interact with this drug include: aliskiren, clonidine, disopyramide, dofetilide, dolasetron, fingolimod, lithium.
Other medications can affect the removal of Hormitol from your body, which may affect how Hormitol works. Examples include erythromycin, rifamycins (such as rifampin), ritonavir, St. John's wort, among others.
Hormitol can slow down the removal of other medications from your body, which may affect how they work. Examples of affected drugs include asunaprevir, colchicine, flibanserin, ivabradine, lomitapide, midazolam, triazolam, among others.
Some products have ingredients that could raise your heart rate or blood pressure. Tell your pharmacist what products you are using, and ask how to use them safely (especially cough-and-cold products, diet aids, or NSAIDs such as ibuprofen/naproxen).
Hormitol may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:
- dizziness or lightheadedness
Patients With Hypertrophic Cardiomyopathy (IHSS)
In 120 patients with hypertrophic cardiomyopathy (most of them refractory or intolerant to propranolol) who received therapy with Hormitol at doses up to 720 mg/day, a variety of serious adverse effects were seen. Three patients died in pulmonary edema; all had severe left ventricular outflow obstruction and a past history of left ventricular dysfunction. Eight other patients had pulmonary edema and/or severe hypotension; abnormally high (greater than 20 mm Hg) pulmonary wedge pressure and a marked left ventricular outflow obstruction were present in most of these patients. Concomitant administration of quinidine (see DRUG INTERACTIONS) preceded the severe hypotension in 3 of the 8 patients (2 of whom developed pulmonary edema). Sinus bradycardia occurred in 11% of the patients, second-degree AV block in 4%, and sinus arrest in 2%. It must be appreciated that this group of patients had a serious disease with a high mortality rate. Most adverse effects responded well to dose reduction, and only rarely did Hormitol use have to be discontinued.
What is the dosage for Hormitol?
Hormitol can be taken with food.
- Angina (immediate release formulations): 80-160 mg three times daily. Angina (extended release formulations): 180-540 mg at bedtime.
- Hypertension (immediate release): 80-320 mg twice daily. Hypertension (extended release): 120-480 mg once or twice daily depending on the brand.
- Migraine: 160-320 mg three to four times daily.