Sildenafil
30mg
Chewable Tablets
Oral durg for treat high blood pressure in the lungsused in animals only
Description:
Sildenafil a highly selective PDE-5 inhibitor, is used to block the inactivation of cGMP by PDE-5, which leads to pulmonary artery vasodilation (McLaughlin and McGoon, 2006). The mechanism of action in animals is similar to that in humans. Sildenafil works by inhibiting phosphodiesterase type 5 (PDE5), which leads to the relaxation of blood vessels and improved blood flow.
Sildenafil is used in dogs and cats to treat pulmonary arterial hypertension (high blood pressure in the blood vessels of the lungs). It is also used to help improve symptoms associated with megaesophagus and myxomatous mitral valve disease in dogs.
The chemical name of Sildenafil is "1-[4-ethoxy-3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-5-yl)phenylsulfonyl]-4-methylpiperazine." The ctural formula of Sildenafil is:
Indications:
Sildenafil is used in veterinary medicine for treating certain conditions in animals, particularly in dogs and cats. The key indications for its use include:
Pulmonary Arterial Hypertension (PAH)
Megaesophagus
Myxomatous Mitral Valve Disease (MMVD) in Dogs
Heart Disease
Pulmonary Disorders
In all these cases, Sildenafil works by inhibiting phosphodiesterase type 5 (PDE5), leading to the relaxation of blood vessels and improved blood flow.
Dosage and Administration:
The dosage and administration of Sildenafil in animals, particularly in dogs and cats, vary based on several factors including the species, size of the animal, the condition being treated, and the individual animal's response to the medication. It's important to note that Sildenafil should only be used in animals under the guidance of a veterinarian. Here are general guidelines:
Dosage:
Dogs: The typical dosage for dogs ranges from 1 to 3 mg per kilogram of body weight, administered two to three times daily.
Cats: In cats, the dosage generally ranges from 0.5 to 1 mg per kilogram of body weight, given two to three times daily.
Administration:
Sildenafil is administered orally and can be given with or without food. However, administering it on an empty stomach might increase its absorption.
The medication comes in tablet form and may need to be cut or crushed for easier administration, depending on the size of the animal and the prescribed dosage.
Frequency:
The frequency of administration is generally two to three times a day, but this can vary based on the veterinarian's assessment and the specific needs of the animal.
Treatment Duration:
The duration of treatment with Sildenafil depends on the condition being treated and how well the animal responds to therapy.
Chronic conditions like pulmonary arterial hypertension may require long-term treatment.
Contraindications:
Sildenafil should not be given in Pre-existing Hypotension, Severe Cardiovascular Disease, Concurrent Nitrate Medication, Severe Liver or Kidney Disease, Recent Stroke or Heart Attack, Known Allergy, Certain Eye Conditions,Breeding Animal.
Warnings:
Warnings for Humans:
Humans should avoid direct contact with Sildenafil, especially if they have a known allergy to it. Wear gloves when handling the medication. Pregnant or nursing women should be particularly cautious, as the effects of accidental ingestion or significant dermal exposure to Sildenafil are not well established.If a human accidentally ingests Sildenafil intended for animal use, they should seek medical attention, especially if any adverse reactions are observed.
Keep Sildenafil out of reach of children and other animals in the household to prevent accidental ingestion.
Warnings for Animals :
Monitoring: Animals being treated with Sildenafil denafil should be closely monitored for any signs of adverse reactions. This includes monitoring blood pressure and watching for symptoms of hypotension, such as weakness or lethargy.
Drug Interactions: Be aware of potential drug interactions. Inform the veterinarian about all other medications and supplements the animal is receiving.
Regular Veterinary Check-ups: Regular check-ups with the veterinarian are important to assess the effectiveness of the treatment and to adjust the dosage as necessary.
Adverse Reactions:
Sildenafil is generally well-tolerated. Rare side effects may include:
Vomiting
Diarrhea
Decrease in appetite
A flush red appearance to the skin, especially around the belly or groin
Clinical Pharmacology:
The clinical pharmacology of Sildenafil when used in animals, particularly dogs and cats, encompasses its pharmacokinetics and pharmacodynamics. Here’s an overview:
Mechanism of Action:
Sildenafil is a phosphodiesterase type 5 (PDE5) inhibitor. It enhances the effects of nitric oxide (NO) by inhibiting PDE5, an enzyme responsible for the breakdown of cyclic guanosine monophosphate (cGMP) in the smooth muscle cells lining the blood vessels supplying various tissues.
Inhibiting PDE5 leads to increased levels of cGMP, resulting in smooth muscle relaxation (vasodilation) and improved blood flow. This mechanism is critical in treating pulmonary arterial hypertension (PAH) and certain cardiac conditions in animals.
Pharmacokinetics:
Absorption: Sildenafil is absorbed from the gastrointestinal tract after oral administration. The presence of food can affect its absorption.
Distribution: It is widely distributed in the body and has a high lipid solubility. It can cross the blood-brain barrier and also reaches the pulmonary system effectively, which is essential for its therapeutic action in PAH.
Metabolism: Sildenafil is metabolized primarily in the liver, involving cytochrome P450 enzymes, predominantly CYP3A4 and CYP2C9.
Excretion: The drug and its metabolites are excreted mainly via feces and urine.
Uses in Veterinary Medicine:
The primary use of Sildenafil in veterinary medicine is for the treatment of pulmonary arterial hypertension. By reducing pulmonary vascular resistance, it eases the cardiac workload and improves symptoms associated with PAH.
It may also be used for heart conditions where pulmonary hypertension is a secondary complication.
Storage Information:
Store this medication at room temperature (around 77°F or 25°C).
Generic medication and its counterpart to have the same active ingredients, strength, quality, route of administration, and safety standards.All of our products are produced in GMP factories, Your pet’s health is our top priority.
This summary contains important information about Sildenafil. You should read this information before you start giving your pet Sildenafil and review it each time the prescription is refilled as there may be new information. This sheet is provided only as a summary and does not take the place of instructions from your veterinarian. Talk with your veterinarian if you do not understand any of this information or if you want to know more about Sildenafil.
What is Sildenafil?
Sildenafil, a highly selective PDE-5 inhibitor, is used to block the inactivation of cGMP by PDE-5, which leads to pulmonary artery vasodilation (McLaughlin and McGoon, 2006). The mechanism of action in animals is similar to that in humans. Sildenafil works by inhibiting phosphodiesterase type 5 (PDE5), which leads to the relaxation of blood vessels and improved blood flow.
Sildenafil is used in veterinary medicine for treating certain conditions in animals, particularly in dogs and cats.Here are the primary uses of Sildenafil in animals:
Pulmonary Arterial Hypertension (PAH):The most common use of Sildenafil in veterinary medicine is for the treatment of pulmonary hypertension (high blood pressure in the arteries of the lungs). Sildenafil helps by dilating the blood vessels in the lungs, which reduces the blood pressure in these vessels and eases the workload on the heart.
Megaesophagus:In dogs with megaesophagus, a condition where the esophagus is enlarged and loses its motility, Sildenafil may be used to manage secondary pulmonary hypertension. Megaesophagus can lead to aspiration pneumonia, which in turn can cause or worsen PAH.
Myxomatous Mitral Valve Disease (MMVD) in Dogs:MMVD, a common heart condition in older dogs, can lead to the development of pulmonary hypertension.
The dosage and administration of Sildenafil in animals are determined by a veterinarian and can vary based on the species, the size of the animal, the specific condition being treated, and the individual response to the medication. It's important to use Sildenafil in animals only under the guidance of a veterinarian.
What are the indications for Sildenafil?
In veterinary medicine, Sildenafil is used off-label for several conditions in animals, particularly in dogs and cats. The main indications include:
Pulmonary Arterial Hypertension (PAH):The most common use of Sildenafil in veterinary medicine is for the treatment of pulmonary hypertension (high blood pressure in the arteries of the lungs). Sildenafil helps by dilating the blood vessels in the lungs, which reduces the blood pressure in these vessels and eases the workload on the heart.
Megaesophagus:In dogs with megaesophagus, a condition where the esophagus is enlarged and loses its motility, Sildenafil may be used to manage secondary pulmonary hypertension. Megaesophagus can lead to aspiration pneumonia, which in turn can cause or worsen PAH.
Myxomatous Mitral Valve Disease (MMVD) in Dogs:MMVD, a common heart condition in older dogs, can lead to the development of pulmonary hypertension.
Heart Disease: In some cases, Sildenafil is used to manage heart disease in animals. It can help improve heart function and exercise tolerance in dogs and cats with certain types of heart conditions.
Pulmonary Disorders: Sildenafil may also be beneficial in treating other pulmonary disorders where vascular resistance is a concern.
In all these cases, Sildenafil works by inhibiting phosphodiesterase type 5 (PDE5), leading to the relaxation of blood vessels and improved blood flow. The exact dosage and administration depend on the specific condition being treated, the size of the animal, and other individual health factors. It's crucial for Sildenafil to be used under the guidance of a veterinarian, as they can determine the appropriate dosage and monitor the pet for any potential side effects. Regular veterinary check-ups are important to assess the effectiveness of the treatment and to adjust the dosage as necessary.
What are the side effects of Sildenafil?
Sildenafil can produce side effects, as with any medication. While it's generally well-tolerated, it's important to monitor for adverse reactions, especially when beginning treatment or adjusting dosages. Common side effects in animals include:
Gastrointestinal Upset: This can manifest as vomiting or diarrhea. Some animals might also experience a decrease in appetite.
Blood Pressure Changes: As Sildenafil works by dilating blood vessels, it can sometimes cause a drop in blood pressure. Signs might include weakness or lethargy, particularly just after taking the medication.
Increased Heart Rate: Some animals may experience a temporary increase in heart rate.
Hyperactivity or Restlessness: Some pets may become more active or seem restless after taking Sildenafil.
Flushed or Reddened Skin: Although less common in animals than in humans, some pets might show signs of flushed skin due to the vasodilation effects of the medication.
Rare Side Effects: In rare cases, more serious side effects can occur. These might include signs of an allergic reaction (such as hives, difficulty breathing, or swelling of the face, lips, tongue, or throat) or priapism (a painful and prolonged erection, which is more of a concern in male animals).
It's important to start with the lowest effective dose and adjust as necessary under the guidance of a veterinarian. If you notice any of these side effects or any other unusual changes in your pet’s behavior or health after starting Sildenafil, contact your veterinarian immediately.
The veterinarian might need to adjust the dosage or try a different treatment approach depending on the severity and type of side effects experienced. Regular check-ups are important to ensure the medication is working as intended and to monitor for any adverse reactions.
What drug interactions should be noted when using Sildenafil?
When using Sildenafil in animals, particularly in veterinary settings for dogs and cats, Certain medications can interact with Sildenafil, altering its effectiveness or increasing the risk of adverse effects. Key drug interactions to note include:
Nitrates: Just like in humans, the combination of Sildenafil with nitrates (often used to treat heart conditions) can cause a significant and dangerous drop in blood pressure. This combination should be avoided.
Alpha-Blockers: Used to treat high blood pressure or prostate conditions, alpha-blockers can cause blood pressure to drop too low when used with Sildenafil.
Other Phosphodiesterase Inhibitors (PDE Inhibitors): Using Sildenafil in conjunction with other PDE inhibitors can enhance the effects and side effects of these drugs, leading to potential cardiovascular issues, hypotension, or priapism.
Certain Antihypertensive Medications: Some blood pressure medications can further lower blood pressure when used with Sildenafil, necessitating careful monitoring and possible dosage adjustments.
CYP3A4 Inhibitors: Drugs that inhibit the CYP3A4 enzyme can decrease the breakdown of Sildenafil, leading to increased concentrations in the body. This includes certain antifungals (like ketoconazole and itraconazole) and some antibiotics (like erythromycin).
HIV Protease Inhibitors: These medications can also increase the concentration of Sildenafil in the blood, leading to an increased risk of Sildenafil -related side effects.
Antacids: The use of antacids may alter the absorption of Sildenafil, potentially affecting its efficacy.
It's important to inform the veterinarian about all the medications and supplements the animal is taking, as this can guide the safe and effective use of Sildenafil. The veterinarian may need to adjust the dosing or closely monitor for side effects if other medications are being used concurrently with Sildenafil. Regular follow-up and monitoring are crucial when managing pets on multiple medications.
What if I miss giving my pet the medication?
You should give the missed dose as soon as you remember and then wait the recommended amount of time between doses. Never give your pet two doses at once or give extra doses.
Are there any potential side effects?
Side effects are uncommon but may include skin flushing in the groin region, and gastrointestinal upset such as decreased appetite, vomiting, and diarrhea. In humans, side effects may include headache, blindness, nosebleeds, deafness, dizziness, indigestion, muscle aches, and nose congestion. The significance of these effects in dogs and cats is unknown.
This short-acting medication should stop working within 24 hours, although can last longer in pets with liver or kidney disease.
Is there any monitoring that needs to be done with this medication?
Blood pressure in the lungs and in the body should be monitored regularly. Monitor your pet to be sure that the medication is working by noting improvements in ability to exercise, cough, breathing effort, or weight gain. Monitor for side effects.
What should I do in case of emergency?
If you suspect an overdose or an adverse reaction to the medication, call your veterinary office immediately. If they are not available, follow their directions in contacting an emergency facility.