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Example Content from MEDITEXT for 224785-90-4:
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ACUTE EXPOSURE INFORMATION
- USES: Vardenafil, a phosphodiesterase (PDE) 5 inhibitor, is used in the treatment of erectile dysfunction.
- PHARMACOLOGY: During sexual stimulation, nitric oxide is released from the nerve endings and endothelial cells in the corpus cavernosum, which activates the enzyme guanylate cyclase producing an increase synthesis of cyclic guanosine monophosphate (cGMP) in the smooth muscle cells of the corpus cavernosum. The cGMP is regulated by both the rates of synthesis and degradation via phosphodiesterase type 5 (PDEs). The tissue concentration of cGMP is regulated by both the rates of synthesis and degradation via phosphodiesterases (PDEs). The most abundant PDE is the cGMP-specific phosphodiesterase type 5 (PDE5); therefore, the inhibition of PDE5 enhances erectile function by increasing the amount of cGMP.
- EPIDEMIOLOGY: Inadvertent ingestion in children occurs but rarely causes serious effects. PDE5s have the potential for abuse and misuse, and may be deliberately ingested with other drugs (eg amphetamines, hallucinogenic amphetamines, GHB, ketamine, amyl nitrate) to enhance sexual experiences.
- TOXICOLOGY: Vardenafil has systemic vasodilatory effects that can produce transient decreases in blood pressure, flushing, or headache. Based on the effects of PDE5 inhibition on the nitric oxide/cyclic guanosine monophosphate pathway, PDE5 inhibition may potentiate the hypotensive effects of nitrates.
- WITH THERAPEUTIC USE
- ADVERSE EVENTS: Headache, flushing, and rhinitis may frequently occur with vardenafil therapy and appears to be dose-related. Other adverse effects that may occur include dizziness, dyspepsia, nausea, vision abnormalities, chest pain, and priapism. In postmarketing experience, seizures, seizure recurrence and transient global amnesia have developed in temporal association with vardenafil.
- WITH POISONING/EXPOSURE
- MILD TO MODERATE TOXICITY: Limited data. Adverse events are anticipated to be similar to events observed with therapeutic use. During clinical trials in healthy volunteers, ingestion of a single 120-mg dose of vardenafil was associated with the development of reversible back pain, myalgias, and vision abnormalities.
- SEVERE TOXICITY: Information is limited. Hemodynamic compromise (eg, tachycardia, hypotension) may develop when combined with nitrates. In postmarketing experience, seizures and global amnesia have a temporal association with vardenafil.
- ABUSE/MISUSE: There have been reports of misuse/abuse with other PDE5 inhibitors and may occur with vardenafil. These agents have been used by younger individuals and combined with club drugs.
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