Levitra

Levitra (Levitra) is an oral therapy for the treatment of erectile dysfunction. It is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). Penile erection is a hemodynamic process initiated by the relaxation of smooth muscle in the corpus cavernosum and its associated arterioles. During sexual stimulation, nitric oxide is released from nerve endings and endothelial cells in the corpus cavernosum. Nitric oxide activates the enzyme guanylate cyclase resulting in increased synthesis of cyclic guanosine monophosphate (cGMP) in the smooth muscle cells of the corpus cavernosum. The cGMP in turn triggers smooth muscle relaxation, allowing increased blood flow into the penis, resulting in erection. The tissue concentration of cGMP is regulated by both the rates of synthesis and degradation via phosphodiesterases (PDEs). The most abundant PDE in the human corpus cavernosum is the cGMPspecific phosphodiesterase type 5 (PDE5); therefore, the inhibition of PDE5 enhances erectile function by increasing the amount of cGMP.

Medicinal name:
  • Vardenafil 10 MG Oral Tablet [Levitra]
  • Vardenafil 20 MG Oral Tablet [Levitra]
  • Vardenafil 2.5 MG Oral Tablet [Levitra]
  • Vardenafil 5 MG Oral Tablet [Levitra]

Levitra - Pharmacology:

Levitra inhibits the cGMP specific phosphodiesterase type 5 (PDE5) which is responsible for degradation of cGMP in the corpus cavernosum located around the penis. Penile erection during sexual stimulation is caused by increased penile blood flow resulting from the relaxation of penile arteries and corpus cavernosal smooth muscle. This response is mediated by the release of nitric oxide (NO) from nerve terminals and endothelial cells, which stimulates the synthesis of cGMP in smooth muscle cells. Cyclic GMP causes smooth muscle relaxation and increased blood flow into the corpus cavernosum. The inhibition of phosphodiesterase type 5 (PDE5) by vardenafil enhances erectile function by increasing the amount of cGMP.

Levitra mini report

Levitra NDA
NDA - A product marketed under an approved New Drug Application
Levitra TABLET, FILM COATED
TABLET, FILM COATED
Levitra HUMAN PRESCRIPTION DRUG
HUMAN PRESCRIPTION DRUG
Levitra global name
vardenafil hydrochloride
Levitra global name
VARDENAFIL HYDROCHLORIDE
Start - Stop data
START DATA:
2003-Apr-23
Start - Stop data
STOP DATA
not occurred

Levitra for patients

LEVITRAÒ (Luh-VEE-Trah)

(vardenafil HCl) Tablets

Read the Patient Information about LEVITRA before you start taking it and again each time you get a refill. There may be new information. You may also find it helpful to share this information with your partner. This leaflet does not take the place of talking with your doctor. You and your doctor should talk about LEVITRA when you start taking it and at regular checkups. If you do not understand the information, or have questions, talk with your doctor or pharmacist.

WHAT IMPORTANT INFORMATION SHOULD YOU KNOW ABOUT LEVITRA?

LEVITRA can cause your blood pressure to drop suddenly to an unsafe level if it is taken with certain other medicines. With a sudden drop in blood pressure, you could get dizzy, faint, or have a heart attack or stroke.

Do not take LEVITRA if you:

· take any medicines called "nitrates."

· use recreational drugs called "poppers" like amyl nitrate and butyl nitrate.

Tell all your healthcare providers that you take LEVITRA. If you need emergency medical care for a heart problem, it will be important for your healthcare provider to know when you last took LEVITRA.

WHAT IS LEVITRA?

LEVITRA is a prescription medicine taken by mouth for the treatment of erectile dysfunction (ED) in men.

ED is a condition where the penis does not harden and expand when a man is sexually excited, or when he cannot keep an erection. A man who has trouble getting or keeping an erection should see his doctor for help if the condition bothers him. LEVITRA may help a man with ED get and keep an erection when he is sexually excited.

LEVITRA does not:

· cure ED

· increase a manís sexual desire

· protect a man or his partner from sexually transmitted diseases, including HIV. Speak to your doctor about ways to guard against sexually transmitted diseases.

· serve as a male form of birth control

LEVITRA is only for men with ED. LEVITRA is not for women or children. LEVITRA must be used only under a doctorís care.

HOW DOES LEVITRA WORK?

When a man is sexually stimulated, his bodyís normal physical response is to increase blood flow to his penis. This results in an erection. LEVITRA helps increase blood flow to the penis and may help men with ED get and keep an erection satisfactory for sexual activity. Once a man has completed sexual activity, blood flow to his penis decreases, and his erection goes away.

WHO CAN TAKE LEVITRA?

Talk to your doctor to decide if LEVITRA is right for you.

LEVITRA has been shown to be effective in men over the age of 18 years who have erectile dysfunction, including men with diabetes or who have undergone prostatectomy.

WHO SHOULD NOT TAKE LEVITRA?

Do not take LEVITRA if you:

· take any medicines called "nitrates" . Nitrates are commonly used to treat angina. Angina is a symptom of heart disease and can cause pain in your chest, jaw, or down your arm.

Medicines called nitrates include nitroglycerin that is found in tablets, sprays, ointments, pastes, or patches. Nitrates can also be found in other medicines such as isosorbide dinitrate or isosorbide mononitrate. Some recreational drugs called "poppers" also contain nitrates, such as amyl nitrate and butyl nitrate. Do not use LEVITRA if you are using these drugs. Ask your doctor or pharmacist if you are not sure if any of your medicines are nitrates.

· you have been told by your healthcare provider to not have sexual activity because of health problems. Sexual activity can put an extra strain on your heart, especially if your heart is already weak from a heart attack or heart disease.

· are allergic to LEVITRA or any of its ingredients. The active ingredient in LEVITRA is called vardenafil. See the end of this leaflet for a complete list of ingredients.

WHAT SHOULD YOU DISCUSS WITH YOUR DOCTOR BEFORE TAKING LEVITRA? Before taking LEVITRA, tell your doctor about all your medical problems, including if you:

· have heart problems such as angina, heart failure, irregular heartbeats, or have had a heart attack. Ask your doctor if it is safe for you to have sexual activity.

· have low blood pressure or have high blood pressure that is not controlled

· have had a stroke

· or any family members have a rare heart condition known as prolongation of the QT interval (long QT syndrome)

· have liver problems

· have kidney problems and require dialysis

· have retinitis pigmentosa, a rare genetic (runs in families) eye disease

· have ever had severe vision loss, or if you have an eye condition called non-arteritic anterior ischemic optic neuropathy (NAION)

· have stomach ulcers

· have a bleeding problem

· have a deformed penis shape or Peyronieís disease

· have had an erection that lasted more than 4 hours

· have blood cell problems such as sickle cell anemia, multiple myeloma, or leukemia

CAN OTHER MEDICATIONS AFFECT LEVITRA?

Tell your doctor about all the medicines you take including prescription and non-prescription medicines, vitamins, and herbal supplements. LEVITRA and other medicines may affect each other.

Always check with your doctor before starting or stopping any medicines. Especially tell your doctor if you take any of the following:

· medicines called nitrates

· medicines called alpha-blockers. These include HytrinÒ (terazosin HCl), FlomaxÒ (tamsulosin HCl), CarduraÒ (doxazosin mesylate), MinipressÒ (prazosin HCl) or UroxatralÒ (alfuzosin HCl). Alpha-blockers are sometimes prescribed for prostate problems or high blood pressure. In some patients the use of PDE5 inhibitor drugs, including LEVITRA, with alpha-blockers can lower blood pressure significantly leading to fainting. You should contact the prescribing physician if alpha-blockers or other drugs that lower blood pressure are prescribed by another healthcare provider.

· medicines that treat abnormal heartbeat. These include quinidine, procainamide, amiodarone and sotalol.

· ritonavir (NorvirÒ) or indinavir sulfate (CrixivanÒ)

· ketoconazole or itraconazole (such as NizoralÒ or SporanoxÒ)

· erythromycin

· other medicines or treatments for ED

HOW SHOULD YOU TAKE LEVITRA?

Take LEVITRA exactly as your doctor prescribes. LEVITRA comes in different doses (2.5 mg, 5 mg, 10 mg, and 20 mg). For most men, the recommended starting dose is 10 mg. Take LEVITRA no more than once a day. Doses should be taken at least 24 hours apart. Some men can only take a low dose of LEVITRA because of medical conditions or medicines they take. Your doctor will prescribe the dose that is right for you.

· If you are older than 65 or have liver problems, your doctor may start you on a lower dose of LEVITRA.

· If you have prostate problems or high blood pressure, for which you take medicines called alpha-blockers, your doctor may start you on a lower dose of LEVITRA.

· If you are taking certain other medicines your doctor may prescribe a lower starting dose and limit you to one dose of LEVITRA in a 72-hour (3 days) period.

Take 1 LEVITRA tablet about 1 hour (60 minutes) before sexual activity. Some form of sexual stimulation is needed for an erection to happen with LEVITRA. LEVITRA may be taken with or without meals.

Do not change your dose of LEVITRA without talking to your doctor. Your doctor may lower your dose or raise your dose, depending on how your body reacts to LEVITRA.

If you take too much LEVITRA, call your doctor or emergency room right away.

WHAT ARE THE POSSIBLE SIDE EFFECTS OF LEVITRA?

The most common side effects with LEVITRA are headache, flushing, stuffy or runny nose, indigestion, upset stomach, or dizziness. These side effects usually go away after a few hours. Call your doctor if you get a side effect that bothers you or one that will not go away.

LEVITRA may uncommonly cause:

· an erection that wonít go away (priapism). If you get an erection that lasts more than 4 hours, get medical help right away. Priapism must be treated as soon as possible or lasting damage can happen to your penis including the inability to have erections.

· color vision changes, such as seeing a blue tinge to objects or having difficulty telling the difference between the colors blue and green.

In rare instances, men taking PDE5 inhibitors (oral erectile dysfunction medicines, including LEVITRA) reported a sudden decrease or loss of vision in one or both eyes. It is not possible to determine whether these events are related directly to these medicines, to other factors such as high blood pressure or diabetes, or to a combination of these. If you experience sudden decrease or loss of vision, stop taking PDE5 inhibitors, including LEVITRA, and call a doctor right away.

These are not all the side effects of LEVITRA. For more information, ask your doctor or pharmacist.

HOW SHOULD LEVITRA BE STORED?

·Store LEVITRA at room temperature between 59° and 86° F (15° to 30° C).

·Keep LEVITRA and all medicines out of the reach of children.

GENERAL INFORMATION ABOUT LEVITRA.

Medicines are sometimes prescribed for conditions other than those described in patient information leaflets. Do not use LEVITRA for a condition for which it was not prescribed. Do not give LEVITRA to other people, even if they have the same symptoms that you have. It may harm them.

This leaflet summarizes the most important information about LEVITRA. If you would like more information, talk with your healthcare provider. You can ask your doctor or pharmacist for information about LEVITRA that is written for health professionals.

For more information you can also visit www.LEVITRA.com, or call 1-866-LEVITRA.

WHAT ARE THE INGREDIENTS OF LEVITRA?

Active Ingredient: vardenafil hydrochloride

Inactive Ingredients: microcrystalline cellulose, crospovidone, colloidal silicon dioxide, magnesium stearate, hypromellose, polyethylene glycol, titanium dioxide, yellow ferric oxide, and red ferric oxide.

orvir (ritonavir) is a trademark of Abbott Laboratories
Crixivan (indinavir sulfate) is a trademark of Merck & Co., Inc.
Nizoral (ketoconazole) is a trademark of Johnson & Johnson
Sporanox (itraconazole) is a trademark of Johnson & Johnson
Hytrin (terazosin HCl) is a trademark of Abbott Laboratories
Flomax (tamsulosin HCl) is a trademark of Yamanouchi Pharmaceutical Co., Ltd.
Cardura (doxazosin mesylate) is a trademark of Pfizer Inc.
Minipress (prazosin HCl) is a trademark of Pfizer Inc.
Uroxatral (alfuzosin HCl) is a trademark of Sanofi-Synthelabo
LEVITRA is a registered trademark of Bayer Aktiengesellschaft and is used under license by GlaxoSmithKline and Schering Corporation.

Levitra Interactions

Effect of other drugs on Levitra

In vitro studies: Studies in human liver microsomes showed that vardenafil is metabolized primarily by cytochrome P450 (CYP) isoforms 3A4/5, and to a lesser degree by CYP2C9. Therefore, inhibitors of these enzymes are expected to reduce vardenafil clearance.

In vivo studies: Cytochrome P450 Inhibitors

Cimetidine (400 mg b.i.d.) had no effect on vardenafil bioavailability (AUC) and maximum concentration (Cmax) of vardenafil when co-administered with 20 mg Levitra in healthy volunteers.

Erythromycin (500 mg t.i.d) produced a 4-fold increase in vardenafil AUC and a 3-fold increase in Cmax when co-administered with Levitra 5 mg in healthy volunteers. It is recommended not to exceed a single 5 mg dose of Levitra in a 24-hour period when used in combination with erythromycin. Ketoconazole (200 mg once daily) produced a 10-fold increase in vardenafil AUC and a 4-fold increase in Cmax when co-administered with Levitra (5 mg) in healthy volunteers. A 5-mg Levitra dose should not be exceeded when used in combination with 200 mg once daily ketoconazole. Since higher doses of ketoconazole (400 mg daily) may result in higher increases in Cmax and AUC, a single 2.5 mg dose of Levitra should not be exceeded in a 24-hour period when used in combination with ketoconazole 400 mg daily.

HIV Protease Inhibitors: Indinavir (800 mg t.i.d.) co-administered with Levitra 10 mg resulted in a 16-fold increase in vardenafil AUC, a 7-fold increase in vardenafil Cmax and a 2-fold increase in vardenafil half-life. It is recommended not to exceed a single 2.5 mg Levitra dose in a 24-hour period when used in combination with indinavir.

Ritonavir (600 mg b.i.d.) co-administered with Levitra 5 mg resulted in a 49-fold increase in vardenafil AUC and a 13-fold increase in vardenafil Cmax. The interaction is a consequence of blocking hepatic metabolism of vardenafil by ritonavir, a highly potent CYP3A4 inhibitor, which also inhibits CYP2C9. Ritonavir significantly prolonged the half-life of vardenafil to 26 hours. Consequently, it is recommended not to exceed a single 2.5 mg Levitra dose in a 72-hour period when used in combination with ritonavir.

Other Drug Interactions: No pharmacokinetic interactions were observed between vardenafil and the following drugs: glyburide, warfarin, digoxin, Maalox, and ranitidine. In the warfarin study, vardenafil had no effect on the prothrombin time or other pharmacodynamic parameters.

Effects of Levitra on other drugs

In vitro studies: Levitra and its metabolites had no effect on CYP1A2, 2A6, and 2E1 (Ki > 100uM). Weak inhibitory effects toward other isoforms (CYP2C8, 2C9, 2C19, 2D6, 3A4) were found, but Ki values were in excess of plasma concentrations achieved following dosing. The most potent inhibitory activity was observed for vardenafil metabolite M1, which had a Ki of 1.4 uM toward CYP3A4, which is about 20 times higher than the M1 Cmax values after an 80 mg Levitra dose.

In vivo studies: Nitrates: The blood pressure lowering effects of sublingual nitrates (0.4 mg) taken 1 and 4 hours after vardenafil and increases in heart rate when taken at 1, 4 and 8 hours were potentiated by a 20 mg dose of Levitra in healthy middle-aged subjects. These effects were not observed when Levitra 20 mg was taken 24 hours before the NTG. Potentiation of the hypotensive effects of nitrates for patients with ischemic heart disease has not been evaluated, and concomitant use of Levitra and nitrates is contraindicated.

Nifedipine: Levitra 20 mg, when co-administered with slow-release nifedipine 30 mg or 60 mg once daily, did not affect the relative bioavailability (AUC) or maximum concentration (Cmax) of nifedipine, a drug that is metabolized via CYP3A4. Nifedipine did not alter the plasma levels of Levitra when taken in combination. In these patients whose hypertension was controlled with nifedipine, Levitra 20 mg produced mean additional supine systolic/diastolic blood pressure reductions of 6/5 mm Hg compared to placebo.

Alpha-blockers: When Levitra 10 or 20 mg was given to healthy volunteers either simultaneously or 6 hours after a 10 mg dose of terazosin, significant hypotension developed in a substantial number of subjects. With simultaneous dosing of Levitra 10 mg and terazosin 10 mg, 6 of 8 subjects experienced a standing systolic blood pressure of less than 85 mm Hg. With simultaneous dosing of Levitra 20 mg and terazosin 10 mg, 2 of 9 subjects experienced a standing systolic blood pressure of less than 85 mm Hg. When Levitra dosing was separated from terazosin 10 mg by 6 hours, 7 of 28 subjects who received 20 mg of Levitra experienced a decrease in standing systolic blood pressure below 85 mm Hg. In a similar study with tamsulosin in healthy volunteers, 1 of 24 subjects dosed with Levitra 20 mg and tamsulosin 0.4 mg separated by 6 hours experienced a standing systolic blood pressure below 85 mm Hg. Two of 16 subjects dosed simultaneously with Levitra 10 mg and tamsulosin 0.4 mg experienced a standing systolic blood pressure below 85 mm Hg. The administration of lower doses of Levitra with alpha-blockers has not been completely evaluated to determine if they can be safely administered together. Based on these data, Levitra should not be used in patients on alpha-blocker therapy.

Ritonavir and indinavir: Upon concomitant administration of 5 mg of Levitra with 600 mg BID ritonavir, the Cmax and AUC of ritonavir were reduced by approximately 20%. Upon administration of 10 mg of Levitra with 800 mg TID indinavir, the Cmax and AUC of indinavir were reduced by 40% and 30%, respectively.

Alcohol: Alcohol (0.5 g/kg body weight: approximately 40 mL of absolute alcohol in a 70 kg person) and vardenafil plasma levels were not altered when dosed simultaneously. Levitra (20 mg) did not potentiate the hypotensive effects of alcohol during the 4-hour observation period in healthy volunteers when administered with alcohol (0.5 g/kg body weight).

Aspirin: Levitra (10 mg and 20 mg) did not potentiate the increase in bleeding time caused by aspirin (two 81 mg tablets).

Other interactions: Levitra had no effect on the pharmacodynamics of glyburide (glucose and insulin concentrations) and warfarin (prothrombin time or other pharmacodynamic parameters).

Levitra Contraindications

Nitrates: Administration of LEVITRA with nitrates (either regularly and/or intermittently) and nitric oxide donors is contraindicated. Consistent with the effects of PDE5 inhibition on the nitric oxide/cyclic guanosine monophosphate pathway, PDE5 inhibitors may potentiate the hypotensive effects of nitrates. A suitable time interval following LEVITRA dosing for the safe administration of nitrates or nitric oxide donors has not been determined.

Hypersensitivity: LEVITRA is contraindicated for patients with a known hypersensitivity to any component of the tablet.

Manufacturers name:

  • GlaxoSmithKline LLC
  • PD-Rx Pharmaceuticals, Inc
  • APHENA PHARMA SOLUTIONS - TENNESSEE, INC
  • KAISER FOUNDATION HOSPITALS
  • Physicians Total Care, Inc
  • Bryant Ranch Prepack

Generic name, Overdose, Half Life Levitra, Food Interactions, Chemical, etc..

Levitra see also FDA report Saw Palmetto

Men's Health

Chemical structure:
N N N N N O N S O O O H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H C23H32N6O4S 2D chemical structure C23H32N6O4S SVG | 2D structure chemical names, chemical properties, classification C23H32N6O4S