Upwardz
Upwardz Uses, Dosage, Side Effects, Food Interaction and all others data.
When sexual stimulation causes the local release of nitric oxide in the corpus cavernosum, then nitric oxide activates the enzyme guanylyl cyclase, which results in increased levels of cGMP. The increased levels of cGMP in the corpus cavernosum produce smooth muscle relaxation and inflow of blood into the penile tissues, thereby producing an erection. PDE5 degrades cGMP in the corpus cavernosum, and the inhibition of PDE5 by Upwardz maintains increased levels of cGMP in the corpus cavernosum. Upwardz has no effect on penile blood flow in absence of sexual stimulation.
Upwardz is used to treat male erectile dysfunction (impotence) and pulmonary arterial hypertension (PAH). Part of the physiological process of erection involves the release of nitric oxide (NO) in the corpus cavernosum. This then activates the enzyme guanylate cyclase which results in increased levels of cyclic guanosine monophosphate (cGMP), leading to smooth muscle relaxation in the corpus cavernosum, resulting in increased inflow of blood and an erection. Upwardz is a potent and selective inhibitor of cGMP specific phosphodiesterase type 5 (PDE5) which is responsible for degradation of cGMP in the corpus cavernosum. This means that, with tadalafil on board, normal sexual stimulation leads to increased levels of cGMP in the corpus cavernosum which leads to better erections. Without sexual stimulation and no activation of the NO/cGMP system, tadalafil should not cause an erection.
Trade Name | Upwardz |
Availability | Prescription only |
Generic | Tadalafil |
Tadalafil Other Names | Tadalafil, Tadalafilo |
Related Drugs | tamsulosin, finasteride, sildenafil, Flomax, prazosin, doxazosin, Viagra, Cialis, alprostadil, Levitra |
Type | Tablet |
Formula | C22H19N3O4 |
Weight | Average: 389.404 Monoisotopic: 389.137556111 |
Protein binding | 94% |
Groups | Approved, Investigational |
Therapeutic Class | Drugs for Erectile Dysfunction |
Manufacturer | Ttk Healthcare Ltd |
Available Country | India |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Upwardz is used for the treatment of erectile dysfunction (ED).
Upwardz is used for the treatment of the signs and symptoms of benign prostatic hyperplasia (BPH).
Upwardz is used for the treatment of erectile dysfunction and the signs of benign prostatic hyperplasia (ED/BPH).
Upwardz is also used to associated treatment for these conditions: Benign Prostatic Hyperplasia (BPH), Erectile Dysfunction, Symptomatic pulmonary arterial hypertension (PAH)
How Upwardz works
Penile erection during sexual stimulation is achieved by the relaxation of penile arteries and corpus cavernosal smooth muscles, leading to increased blood flow to the organ. 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, and is degraded by the cGMP specific phosphodiesterase type 5 (PDE5) in the corpus cavernosum located around the penis. Upwardz inhibits PDE5 and thereby enhances erectile function by increasing the amount of cGMP available.
Dosage
Upwardz dosage
Erectile Dysfunction-
For Use as Needed:
- The recommended starting dose of Upwardz for use as needed in most patients is 10 mg, taken prior to anticipated sexual activity.
- The dose may be increased to 20 mg or decreased to 5 mg, based on individual efficacy and tolerability. The maximum recommended dosing frequency is once per day in most patients.
For Once Daily Use:
- The recommended starting dose of Upwardz for once daily use is 2.5 mg, taken at approximately the same time every day, without regard to timing of sexual activity.
- The Upwardz dose for once daily use may be increased to 5 mg, based on individual efficacy and tolerability.
Patients with BPH or with ED and BPH-
- Intimate for once daily use for BPH: The recommended dose of Intimate for once daily use is 5 mg, taken at approximately the same time every day.
- Intimate for once daily use for ED+BPH: The recommended dose of Intimate for once daily use is 5 mg, taken at approximately the same time every day, without regard to timing of sexual activity.
Upwardz may be taken without regard to food.
Side Effects
Body as a whole: hypersensitivity reactions including rash, urticaria, facial edema, Stevens-Johnson syndrome, and exfoliative dermatitis.
Cardiovascular and cerebrovascular: Serious cardiovascular events, including myocardial infarction, sudden cardiac death, unstable angina pectoris, ventricular arrhythmia, stroke, transient ischemic attacks, chest pain, palpitations, and tachycardia, may occur. Most of the patients in whom these events have been reported had pre-existing cardiovascular risk factors. Hypotension (more commonly reported when tadalafil is given to patients who are already taking antihypertensive agents), hypertension, and syncope.
Skin and subcutaneous tissues: hyperhidrosis (sweating).
Gastrointestinal: abdominal pain and gastroesophageal reflux.
Nervous system: migraine, transient global amnesia.Respiratory system: epistaxis (nose bleed).
Special senses: blurred vision, nonarteritic anterior ischemic optic neuropathy, retinal vein occlusion, visual field defect.
Otologic: cases of sudden decrease or loss of hearing have been reported.
Toxicity
Oral, Rat LD50 = 2000 mg/kg, no deaths or toxicity.
Precaution
Cardiovascular: Physicians should consider the cardiovascular status of their patients, since there is a degree of cardiac risk associated with sexual activity. Potential for Drug Interactions When Taking Upwardz for Once Daily Use Physicians should be aware that Upwardz for once daily use provides continuous plasma Upwardz levels and should consider this when evaluating the potential for interactions with medications (e.g., nitrates, alpha-blockers, anti-hypertensives and potent inhibitors of CYP3A4).
Prolonged Erection: There have been rare reports of prolonged erections greater than 4 hours and priapism (painful erections greater than 6 hours in duration) for this class of compounds. Priapism, if not treated promptly, can result in irreversible damage to the erectile tissue. Patients who have an erection lasting greater than 4 hours, whether painful or not, should seek emergency medical attention. Upwardz should be used with caution in patients who have conditions that might predispose them to priapism (such as sickle cell anemia, multiple myeloma, or leukemia), or in patients with anatomical deformation of the penis (such as angulation, cavernosal fibrosis, or Peyronie’s disease).
Eye & Sudden Hearing Loss: Physicians should advise patients to stop use of all PDE5 inhibitors, including Upwardz, and seek medical attention in the event of a sudden loss of vision in one or both eyes & sudden decrease or loss of hearing.
Alpha blockers and Antihypertensives: Physicians should discuss with patients the potential for Upwardz to augment the blood-pressure-lowering effect of alpha blockers and antihypertensive medications. Caution is advised when PDE5 inhibitors are coadministered with alpha blockers Renal Insufficiency, Hepatic Impairment, Consumption of alcohol.
Food Interaction
- Avoid excessive or chronic alcohol consumption. Ingesting excess amounts of alcohol (more than four drinks in a short time) may potentiate the hypotension and dizziness caused by tadalafil.
- Avoid grapefruit products. Upwardz is metabolized by CYP3A4, and grapefruit products are CYP3A4 inhibitors; therefore, coadministration may increase serum levels of tadalafil and result in increased hypotension.
- Take with or without food.
[Moderate] GENERALLY AVOID: Additive hypotensive effects may occur when phosphodiesterase-5 (PDE5) inhibitors such as tadalafil are used with alcohol, as both are mild systemic vasodilators.
In clinical pharmacology studies, more subjects administered alcohol at a dose of 0.7 g
There were reports of postural dizziness, and orthostatic hypotension was observed in some.
When tadalafil 20 mg was administered with alcohol at a lower dose of 0.6 g
Neither tadalafil nor alcohol affected the plasma concentrations of the other.
GENERALLY AVOID: Coadministration with grapefruit juice is likely to increase the plasma concentrations of tadalafil, which is primarily metabolized by CYP450 3A4.
However, the interaction has not been studied.
The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit.
MANAGEMENT: Patients taking tadalafil should avoid consuming large amounts of alcohol, which may increase the potential for orthostatic signs and symptoms including increase in heart rate, decrease in standing blood pressure, dizziness, and headache.
It may also be appropriate to avoid consuming large amounts of grapefruit juice.
Upwardz Drug Interaction
Major: sildenafilMinor: tamsulosin, metoprolol, metoprololUnknown: aspirin, aspirin, ubiquinone, rosuvastatin, duloxetine, apixaban, omega-3 polyunsaturated fatty acids, fluticasone nasal, atorvastatin, pregabalin, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol, rivaroxaban, cetirizine
Upwardz Disease Interaction
Major: cardiovascular disease, renal dysfunction, pulmonary diseaseModerate: priapism, alcoholism, hearing loss, liver disease, retinitis pigmentosa, seizure disorders
Volume of Distribution
- 63 L
Elimination Route
After single oral-dose administration, the maximum observed plasma concentration (Cmax) of tadalafil is achieved between 30 minutes and 6 hours (median time of 2 hours). Absolute bioavailability of tadalafil following oral dosing has not been determined.
Half Life
17.5 hours
Clearance
- oral cl=2.5 L/hr
Elimination Route
Upwardz is excreted predominantly as metabolites, mainly in the feces (approximately 61% of the dose) and to a lesser extent in the urine (approximately 36% of the dose).
Pregnancy & Breastfeeding use
It is not indicated for use in newborn, children or women.
Contraindication
Nitrates: Administration of tadalafil to patients who are using any form of organic nitrate, either regularly and/or intermittently, is contraindicated. In clinical pharmacology studies, tadalafil was shown to potentiate the hypotensive effect of nitrates.
Hypersensitivity Reactions: Upwardz is contraindicated in patients with a known serious hypersensitivity to tadalafil. Hypersensitivity reactions have been reported, including Stevens-Johnson syndrome and exfoliative dermatitis.
Special Warning
Renal Insufficiency-
For Use as Needed:
- Mild (creatinine clearance 51 to 80 mL/min): No dose adjustment is required.
- Moderate (creatinine clearance 31 to 50 mL/min): A starting dose of 5 mg not more than once per day is recommended, and the,maximum dose should be limited to 10 mg not more than once in every 48 hours.
- Severe (creatinine clearance <30 mL/min and on hemodialysis): The maximum recommended dose is 5 mg not more than once in every 72 hours.
For Once Daily Use:
- Mild (creatinine clearance 51 to 80 mL/min): No dose adjustment is required. Moderate (creatinine clearance 31 to 50 mL/min): No dose adjustment is required.
- Severe (creatinine clearance <30 mL/min and on hemodialysis): Upwardz for once daily use is not recommended.
Hepatic Impairment-
For Use as Needed:
- Mild or moderate: The dose should not exceed 10 mg once per day.
- Severe: Not recommended
For Once Daily Use:
- Mild or moderate: Upwardz for once daily use has not been extensively evaluated in patients with hepatic insufficiency. Therefore, caution is advised if Upwardz for once daily use is prescribed to these patients.
- Severe: Not recommended.
Geriatrics:
No dose adjustment is required in patients >65 years of age
Acute Overdose
Adverse events were similar to those seen at lower doses. In case of overdose, standard supportive measure should be adopted as required
Storage Condition
Store below 30° C. Protect from light and moisture. Keep out of reach of children.
Innovators Monograph
You find simplified version here Upwardz
Upwardz contains Tadalafil see full prescribing information from innovator Upwardz Monograph, Upwardz MSDS, Upwardz FDA label
FAQ
What is Upwardz used for?
Upwardz used to treat erection problems (erectile dysfunction) and symptoms of an enlarged prostate (benign prostate enlargement). It's also sometimes used to treat pulmonary hypertension (high blood pressure in the blood vessels that supply the lungs).
What are the side effects of Upwardz?
Many men do not have any side effects from Upwardz while some have mild side effects. These may include headaches, back pain, muscle aches, pain in your arms and legs, facial flushes, stuffy nose, and indigestion. Do not take Upwardz if you also take medicines called nitrates (often prescribed for chest pain)
How long do Upwardz side effects last?
These side effects usually go away after a few hours. Men who get back pain and muscle aches usually get it 12 to 24 hours after taking Cialis. Back pain and muscle aches usually go away within 2 days.
Is Upwardz bad for your heart?
This medicine can cause serious side effects in patients with heart problems. Do not use this medicine if you are also using riociguat or a nitrate medicine, often used to treat angina (chest pain).
Does Upwardz affect the heart?
This will increase the supply of blood to the lungs and reduce the workload of the heart.
Does Upwardz make you last longer?
Recent studies have suggested that the drug's active ingredient.Upwardz might have some efficacy in delaying orgasm.Cialis is not a licensed treatment for premature ejaculation and should not be used as such.
Is Upwardz safe during pregnancy ?
Use should be avoided.Upwardz is not recommended in pregnancy.
Is Upwardz safe during breastfeeding?
Upwardz is not recommended while breastfeeding time.
Is Upwardz safe to take?
Upwardz at doses of 5, 10, or 20mg taken as needed up to once daily for 18 to 24 months was safe and well tolerated. These findings support the long-term use of Upwardz in the clinical management of erectile dysfunction.
Who should not take Upwardz?
Upwardz can only be taken by adults aged 18 and over.Upwardz is not suitable for some people. Do not take Upwardz if you have had an allergic reaction to Upwardz or any other medicines in the past.
Can I take alcohol with Upwardz ?
combining it with alcohol may further increase this effect. You may be more likely to experience symptoms such as dizziness, lightheadedness, fainting, flushing, headache, and heart palpitations.
Can I take Upwardz long time Upwardz?
Upwardz taken as needed up to once daily for 18 to 24 months was safe and well tolerated. These findings support the long-term use of Upwardz in the clinical management of erectile dysfunction.
Is Upwardz safe for liver?
Upwardz may not harmful for liver.It has not been linked to cases of acute liver failure, chronic hepatitis or vanishing bile duct syndrome.
Can Upwardz raise blood pressure?
While Upwardz does have the potential to lower blood pressure, the effects are typically not cause for concern in healthy men. In certain cases, however, medical conditions and drugs can increase Upwardz hypotensive effects sometimes to a dangerous level.
Can Upwardz be taken daily?
Upwardz is one of the most popular erectile dysfunction drugs. The drug comes in low-dose versions that can be taken daily.
Does Upwardz slow heart rate?
Upwardz works on the enzyme in the lungs to relax the blood vessels. This will increase the supply of blood to the lungs and reduce the workload of the heart.
How do you take Upwardz for best results?
You should take one tablet at least half an hour before you plan to have sex (it may still be effective up to 36 hours after taking the tablet). Do not take more than one dose in 24 hours.
What happens if take too much Upwardz?
If you take too much Upwardz or take it together with these medicines, the chance for side effects will be higher. If you experience a prolonged erection for more than 4 hours or a painful erection for more than 6 hours, contact your doctor immediately.
Can I cut Upwardz in half?
Do not break or split a Cialis tablet. Take the medicine at the same time each day, with or without food. Do not change your Upwardz dose or stop taking this medicine without your doctor's advice.
Why is Upwardz not working?
If Upwardz does not work for you, it may be because: you have not waited long enough after taking it before trying to have sex. you have waited too long after taking it to have sex. the dose is not high enough.