Revatio

Name: Revatio

What is sildenafil, and how does it work (mechanism of action)?

Viagra (sildenafil) is an oral drug that is used for treating impotence (or erectile disfunction, ED, the inability to attain or maintain a penile erection). It is in a class of drugs called phosphodiesterase inhibitors (PDE-5 inhibitors) that also includes

  • tadalafil (Cialis),
  • vardenafil (Levitra, Staxyn ODT), and
  • avanafil (Stendra).

It has been estimated that impotence affects 140 million men worldwide. Over half of all men with impotence are thought to have some physical (medical) cause. The remainder are believed to have psychogenic causes of impotence. Medical causes of impotence include diabetes and circulatory, neurological, or urological conditions.

Penile erection is caused by the engorgement of the penis with blood. This engorgement occurs when the blood vessels delivering blood to the penis increase the delivery of blood and the blood vessels carrying blood away from the penis decrease the removal of blood. Under normal conditions, sexual stimulation leads to the production and release of nitric oxide in the penis. Nitric oxide then activates the enzyme, guanylate cyclase, which causes the production of cyclic guanosine monophosphate (cGMP). It is the cGMP that is primarily responsible for the erection by affecting the amount of blood that the blood vessels deliver and remove from the penis.

Viagra inhibits an enzyme called phosphodiesterase-5 (PDE5) which destroys the cGMP. Thus, Viagra prevents the destruction of cGMP and allows cGMP to accumulate and persist longer. The longer cGMP persists, the more prolonged the engorgement of the penis. The FDA approved Viagra in March 1998.

Do I need a prescription for sildenafil?

Yes

What is the dosage for sildenafil?

  • The usual recommended dose is 25 to 100 mg 1 hour before sexual activity.
  • The maximum dose is 100 mg daily.
  • The elderly (over 65 years of age) should start at 25 mg before sexual activity.
  • Sildenafil is rapidly absorbed. Maximum observed plasma concentrations are reached within 30 to 120 minutes (median 60 minutes) of oral dosing in the fasted state. When sildenafil is taken with a high fat meal, the rate of absorption is reduced, with an average delay in the time to maximal concentration of 1 hour.

How supplied

Dosage Forms And Strengths

REVATIO Tablets

White, film-coated, round tablets engraved with “RVT20” containing sildenafil citrate equivalent to 20 mg of sildenafil.

REVATIO Injection

Single use vial containing 10 mg/12.5 mL of sildenafil.

REVATIO For Oral Suspension

White to off-white powders containing 1.57 g of sildenafil citrate (equivalent to 1.12 g of sildenafil) in a bottle intended for constitution. Following constitution with 90 mL of water, the volume of the oral suspension is 112 mL and the oral suspension contains 10 mg/mL sildenafil. A 2 mL oral syringe (with 0.5 mL and 2 mL dose markings) and a press-in bottle adaptor are also provided.

Storage And Handling

REVATIO tablets are supplied as white, film-coated, round tablets containing sildenafil citrate equivalent to the nominally indicated amount of sildenafil as follows:

REVATIO Tablets
Package Configuration Strength NDC Engraving on Tablet
Bottle of 90 Tablets 20 mg 0069-4190-68 RVT20

Recommended Storage for REVATIO Tablets: Store at controlled room temperature 20°C - 25°C (68°F - 77°F) ; excursions permitted to 15°C - 30°C (59°F -86°F) [see USP Controlled Room Temperature].

REVATIO injection is supplied as a clear, colorless, sterile, ready to use solution containing 10 mg sildenafil/12.5 mL presented in a single-use glass vial.

REVATIO Injection
Package Configuration Strength NDC
Vial individually packaged in a carton 10 mg /12.5 mL 0069-0338-01

Recommended Storage for REVATIO Injection: Store at controlled room temperature 20°C - 25°C (68°F -77°F); excursions permitted to 15°C - 30°C (59°F - 86°F) [see USP Controlled Room Temperature].

REVATIO powder for oral suspension is supplied in amber glass bottles. Each bottle contains white to off-white powders containing 1.57 g of sildenafil citrate (equivalent to 1.12 g sildenafil). Following constitution, the volume of the oral suspension is 112 mL (10 mg sildenafil/mL). A 2 mL oral dosing syringe (with 0.5 mL and 2 mL dose markings) and a press-in bottle adaptor are also provided.

REVATIO Powder for Oral Suspension
Package Configuration Strength NDC
Powder for oral suspension - bottle 10 mg/mL (when reconstituted) 0069-0336-21

Recommended storage for REVATIO for oral suspension: Store below 30°C (86°F) in the original package in order to protect from moisture.

Constituted Oral Suspension Store below 30°C (86°F) or in refrigerator at 2°C to 8°C (36° F - 46°F). Do not freeze. The shelf-life of the constituted oral suspension is 60 days. Any remaining oral suspension should be discarded 60 days after constitution.

Distributed by: Pfizer, Pfizer Labs, Division of Pfizer Inc, NY, NY 10017. Revised: April 2015

What should i avoid while taking oral sildenafil (revatio, viagra)?

Drinking alcohol can increase certain side effects of sildenafil.

Avoid using other medicines to treat impotence, such as alprostadil (Caverject, Muse, Edex) or yohimbine (Yocon, Yodoxin, others), without first talking to your doctor.

Breastfeeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Other Interactions

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following may cause an increased risk of certain side effects but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.

  • Grapefruit Juice
  • Pomelo Juice

Revatio Usage

Revatio comes in tablet and oral suspension (liquid) form and is taken taken 3 times a day, 4-6 hours apart.To prepare the oral solution:

  1. Tap the bottle to release the powder.
  2. Remove the cap.
  3. Accurately measure out 60 mL of water and pour the water into the bottle.
  4. Replace the cap and shake the bottle vigorously for a minimum of 30 seconds.
  5. Remove the cap.
  6. Accurately measure out another 30 mL of water and add this to the bottle. You should always add a total of 90 mL of water irrespective of the dose prescribed.
  7. Replace the cap and shake the bottle vigorously for a minimum of 30 seconds.
  8. Remove the cap.
  9. Press the bottle adaptor into the neck of the bottle. The adaptor is provided so that you can fill the oral syringe with medicine from the bottle. Replace the cap on the bottle.
  10. Write the expiration date of the constituted oral suspension on the bottle label (the expiration date of the constituted oral suspension is 30 days from the date of constitution).

This medication is available in an injectable form to be given directly into a vein (IV) by a healthcare professional.

Revatio Dosage

For the treatment of pulmonary arterial hypertension (PAH):

Revatio tablets and oral solution: The recommended dose of Revatio (sildenafil) is 20 mg three times a day. Take Revatio doses 4–6 hours apart. Doses higher than 20 mg three times a day is not recommended.

Injectable: The recommended dose is 10 mg (12.5 mL) given as an injection into the vein (IV) three times a day.

What is the most important information I should know about oral sildenafil?

Some medicines can cause unwanted or dangerous effects when used with sildenafil. Tell your doctor about all your current medicines, especially riociguat (Adempas).

Do not take sildenafil if you are also using a nitrate drug for chest pain or heart problems, including nitroglycerin, isosorbide dinitrate, isosorbide mononitrate, and some recreational drugs such as "poppers". Taking sildenafil with a nitrate medicine can cause a sudden and serious decrease in blood pressure.

Contact your doctor or seek emergency medical attention if your erection is painful or lasts longer than 4 hours. A prolonged erection (priapism) can damage the penis.

Stop using sildenafil and get emergency medical help if you have sudden vision loss.

Proper Use of sildenafil

This section provides information on the proper use of a number of products that contain sildenafil. It may not be specific to Revatio. Please read with care.

Use sildenafil exactly as directed by your doctor. Do not use more of it and do not use it more often than your doctor ordered. If too much is used, the chance of side effects is increased.

Special patient instructions comes with sildenafil. Read the directions carefully before you start using sildenafil and each time you get a refill of your medicine.

You may take this medicine with or without food.

If you are using the oral liquid, shake the bottle well for at least 10 seconds before measuring each dose. Use the oral syringe provided in the package to measure each dose. Wash the oral syringe after each use.

This medicine usually begins to work for erectile dysfunction within 30 minutes after taking it. It continues to work for up to 4 hours, although its action is usually less after 2 hours.

Use only the brand of this medicine that your doctor prescribed. Different brands may not work the same way.

Dosing

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

  • For treatment of erectile dysfunction:
    • For oral dosage form (tablets):
      • Adults up to 65 years of age—50 milligrams (mg) as a single dose no more than once a day, 1 hour before sexual intercourse. Alternatively, the medicine may be taken 30 minutes to 4 hours before sexual intercourse. Your doctor may adjust your dose if needed.
      • Adults 65 years of age and older—25 mg as a single dose no more than once a day, 1 hour before sexual intercourse. Alternatively, the medicine may be taken 30 minutes to 4 hours before sexual intercourse. Your doctor may adjust your dose if needed.
      • Children—Use is not recommended.
  • For treatment of pulmonary arterial hypertension:
    • For oral dosage forms (suspension or tablets):
      • Adults—5 or 20 milligrams (mg) three times a day. Each dose should be taken about 4 to 6 hours apart.
      • Children—Use and dose must be determined by your doctor.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Throw away any unused mixed Revatio® oral liquid after 60 days.

Consumer Information Use and Disclaimer

  • If your symptoms or health problems do not get better or if they become worse, call your doctor.
  • Do not share your drugs with others and do not take anyone else's drugs.
  • Keep a list of all your drugs (prescription, natural products, vitamins, OTC) with you. Give this list to your doctor.
  • Talk with the doctor before starting any new drug, including prescription or OTC, natural products, or vitamins.
  • Some drugs may have another patient information leaflet. Check with your pharmacist. If you have any questions about this medicine, please talk with your doctor, nurse, pharmacist, or other health care provider.
  • 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.

This information should not be used to decide whether or not to take Revatio or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to Revatio. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.

Review Date: October 4, 2017

Revatio Dosage and Administration

Revatio Tablets and Oral Suspension

The recommended dose of Revatio is 5 mg or 20 mg three times a day. Administer Revatio doses 4–6 hours apart.

In the clinical trial no greater efficacy was achieved with the use of higher doses. Treatment with doses higher than 20 mg three times a day is not recommended.

Revatio Injection

Revatio injection is for the continued treatment of patients with PAH who are currently prescribed oral Revatio and who are temporarily unable to take oral medication.

The recommended dose is 2.5 mg or 10 mg administered as an intravenous bolus injection three times a day. The dose of Revatio injection does not need to be adjusted for body weight.

A 10 mg dose of Revatio injection is predicted to provide pharmacological effect of sildenafil and its N-desmethyl metabolite equivalent to that of a 20 mg oral dose.

Reconstitution of the Powder for Oral Suspension

  1. Tap the bottle to release the powder.
  2. Remove the cap.
  3. Accurately measure out 60 mL of water and pour the water into the bottle. (Figure 1)

    Figure 1

  4. Replace the cap and shake the bottle vigorously for a minimum of 30 seconds. (Figure 2)

    Figure 2

  5. Remove the cap.
  6. Accurately measure out another 30 mL of water and add this to the bottle. You should always add a total of 90 mL of water irrespective of the dose prescribed. (Figure 3)

    Figure 3

  7. Replace the cap and shake the bottle vigorously for a minimum of 30 seconds. (Figure 4)

    Figure 4

  8. Remove the cap.
  9. Press the bottle adaptor into the neck of the bottle (as shown on Figure 5, below). The adaptor is provided so that you can fill the oral syringe with medicine from the bottle. Replace the cap on the bottle.

    Figure 5

  10. Write the expiration date of the constituted oral suspension on the bottle label (the expiration date of the constituted oral suspension is 60 days from the date of constitution).

Incompatibilities

Do not mix with any other medication or additional flavoring agent.

Contraindications

Revatio is contraindicated in patients with:

  • Concomitant use of organic nitrates in any form, either regularly or intermittently, because of the greater risk of hypotension [see Warnings and Precautions (5.2)].
  • Concomitant use of riociguat, a guanylate cyclase stimulator. PDE-5 inhibitors, including sildenafil, may potentiate the hypotensive effects of riociguat.
  • Known hypersensitivity to sildenafil or any component of the tablet, injection, or oral suspension. Hypersensitivity, including anaphylactic reaction, anaphylactic shock and anaphylactoid reaction, has been reported in association with the use of sildenafil.

Revatio dosing information

Usual Adult Dose for Pulmonary Hypertension:

Revatio:
Oral:
-Initial dose: 5 or 20 mg orally three times a day, 4 to 6 hours apart
-Maximum dose: 20 mg orally three times a day

Injection:
-Initial dose: 2.5 or 10 mg IV bolus three times a day

Comments:
-No greater efficacy was achieved with oral doses higher than the maximum recommended dose.
-A 10 mg injection dose is predicted to provide pharmacological effect equivalent to the 20 mg oral dose.

Use: Treatment of PAH (WHO Group I) in adults to improve exercise ability and delay clinical worsening

For Healthcare Professionals

Applies to sildenafil: intravenous solution, oral suspension, oral tablet

General

The most common adverse reactions reported in clinical trials are headache, flushing, dyspepsia, abnormal vision, nasal congestion, back pain, myalgia, nausea, dizziness, and rash.[Ref]

Cardiovascular

Very common (10% or more): Flushing (10%)
Uncommon (0.1% to 1%): Heart rate increased, palpitations, tachycardia, hypertension, hypotension
Rare (less than 0.1%): Myocardial infarction, atrial fibrillation, sudden cardiac death, ventricular arrhythmia, unstable angina
Frequency not reported: Ventricular arrhythmia, sudden cardiac death, angina pectoris, AV block, tachycardia, palpitation, hypotension, postural hypotension, myocardial ischemia, cerebral thrombosis, cardiac arrest, heart failure, abnormal electrocardiogram, cardiomyopathy, shock
Postmarketing reports: Serious cardiovascular, cerebrovascular, and vascular events, including myocardial infarction; sudden cardiac death; ventricular arrhythmia; cerebrovascular hemorrhage; transient ischemic attack; hypertension; subarachnoid, intracerebral, and pulmonary hemorrhage have been reported in temporal association with the use of this drug.[Ref]

Gastrointestinal

Very common (10% or more): Dyspepsia (up to 17%), diarrhea
Common (1% to 10%): Nausea, vomiting, dry mouth, gastritis, gastroesophageal reflux disease, hemorrhoids, abdominal distension
Rare (less than 0.1%): Oral hypoesthesia
Frequency not reported: Glossitis, colitis, dysphagia, gastroenteritis, esophagitis, stomatitis, gingivitis[Ref]

Musculoskeletal

Very common (10% or more): Pain in extremity
Common (1% to 10%): Back pain, myalgia
Frequency not reported: Arthritis, arthrosis, myalgia, tendon rupture, tenosynovitis, bone pain, myasthenia, synovitis[Ref]

Nervous system

Very common (10% or more): Headache (up to 28%)
Common (1% to 10%): Dizziness, migraine, tremor, paresthesia, burning sensation
Uncommon (0.1% to 1%): Somnolence, hypoesthesia
Rare (less than 0.1%): Cerebrovascular accident, syncope
Frequency not reported: Transient ischemic attack, seizure, seizure recurrence, ataxia, hypertonia, neuralgia, neuropathy, paresthesia, somnolence, reflexes decreased
Postmarketing reports: Transient global amnesia[Ref]

Ocular

Very common (10% or more): Abnormal vision (up to 11%)
Common (1% to 10%): Visual color distortion, retinal hemorrhage, visual impairment, vision blurred, photophobia, chromatopsia, cyanopsia, eye irritation, ocular hyperemia
Uncommon (0.1% to 1%): Conjunctival disorders, eye disorders, eye pain, lacrimation disorders, visual acuity reduced, diplopia, abnormal sensation in eye, photopsia, visual brightness, conjunctivitis
Rare (less than 0.1%): Retinal hemorrhage, arteriosclerotic retinopathy, retinal disorder, glaucoma, visual field defect, myopia, asthenopia, vitreous floaters, iris disorder, mydriasis, halo vision, eye edema, eye swelling, eyelid edema, scleral discoloration
Frequency not reported: Non-arteritic anterior ischemic optic neuropathy (NAION), retinal vascular occlusion, visual field defect, cataract[Ref]

This drug has lesser affinity for isoenzyme PDE6, an enzyme found in the retina. This lower selectivity is thought to be the basis for abnormalities related to color vision observed with higher doses or plasma levels.

Nonarteritic anterior ischemic optic neuropathy developed in one eye within minutes to hours after ingestion of sildenafil. Four of the five patients had no vascular risk factors for ischemic optic neuropathy.

-Abnormal Vision: Mild to moderate and transient, predominantly color tinge to vision, but also increased sensitivity to light, or blurred vision.
-Visual color distortions: Chloropsia, chromatopsia, cyanopsia, erythropsia and xanthopsia
-Lacrimation disorders: Dry eye, lacrimal disorder and lacrimation increased[Ref]

Respiratory

Very common (10% or more): Pharyngitis (18%), rhinitis
Common (1% to 10%): Nasal congestion, epistaxis, cough
Uncommon (0.1% to 1%): Sinus congestion
Rare (less than 0.1%): Throat tightness, nasal edema, nasal dryness
Frequency not reported: Asthma, dyspnea, laryngitis, pharyngitis, sinusitis, bronchitis, sputum increased, cough increased[Ref]

Dermatologic

Common (1% to 10%): Rash, alopecia, erythema, night sweats
Frequency not reported: Steven-Johnson syndrome (SJS), toxic epidermal necrolysis(TEN), urticaria, herpes simplex, pruritus, sweating, skin ulcer, contact dermatitis, exfoliative dermatitis[Ref]

Hematologic

Common (1% to 10%): Anemia
Frequency not reported: Leukopenia
Postmarketing reports: In patients with pulmonary arterial hypertension (secondary to sickle cell disease) taking Revatio (R), vaso-occlusive crises requiring hospitalization were more commonly reported. The clinical relevance of this finding in male patients treated with sildenafil (the active ingredient contained in Revatio) for erectile dysfunction is unknown.[Ref]

Metabolic

Common (1% to 10%): Fluid retention
Frequency not reported: Thirst, edema, gout, unstable diabetes, hyperglycemia, hyperuricemia, hypoglycemic reaction, hypernatremia[Ref]

Other

Common (1% to 10%): Cellulitis, influenza, bronchitis, sinusitis, rhinitis, gastroenteritis, vertigo, pyrexia
Uncommon (0.1% to 1%): Tinnitus, chest pain, fatigue, gynecomastia
Rare (less than 0.1%): Deafness, irritability
Frequency not reported: Sudden hearing loss, edema, face edema, peripheral edema, pain, chills accidental fall, accidental injury[Ref]

Psychiatric

Common (1% to 10%): Insomnia, anxiety
Frequency not reported: Abnormal dreams, depression[Ref]

Genitourinary

Uncommon (0.1% to 1%): Penile hemorrhage, hematospermia
Frequency not reported: Priapism, prolonged erection, increased erection, cystitis, nocturia, urinary frequency, urinary incontinence, abnormal ejaculation, genital edema, anorgasmia[Ref]

Renal

Uncommon (0.1% to 1%): Hematuria[Ref]

Hypersensitivity

Rare (less than 0.1%): Hypersensitivity reactions, including rash and urticaria[Ref]

Hepatic

Frequency not reported: Liver function tests abnormal[Ref]

Some side effects of Revatio may not be reported. Always consult your doctor or healthcare specialist for medical advice. You may also report side effects to the FDA.

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