Pilocarpine
PFK Obnovlenie
1190 Items
2019-09-19
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Clinical Pharmacology
With systemic use increases the secretion of salivary, lacrimal, sweat glands, pancreas, intestinal glands, as well as mucosal cells of the respiratory tract.
Indications
For use in ophthalmology: acute glaucoma, secondary glaucoma (thrombosis of the central retinal vein, acute obstruction of the arteries of the retina, optic nerve atrophy, pigmentary retinal degeneration), chronic open-angle glaucoma, corneal abscess. The need for constriction of the pupil after instillation of mydriatics.
Composition
Active ingredient: pilocarpine hydrochloride 10 mg.
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Dosage and Administration
Assign 1 drop of the drug Fotil in the affected eye 2 times / day.
In some patients, a steady decrease in intraocular pressure is achieved only after several weeks of therapy. Therefore, when evaluating the results of treatment, intraocular pressure should be measured approximately 4 weeks after the start of treatment. If the expected reduction in intraocular pressure does not occur, then Fotil forte should be prescribed (Fotil forte drops eye flu. 5 ml box 1 Santen AO) or, given that further dose increases do not have an effect, you should use a combination therapy with inhibitors of carbonic anhydrase for systemic use.
Before starting treatment with Fotil, treatment with other antiglaucoma eye drops should be discontinued the day before.
Adverse reactions
Local reactions: blurred vision, eye irritation, rapid burning sensation and pain in the eye, increased watery eyes, dry eye syndrome, eyelid dermatitis, conjunctivitis redness, ciliary muscle spasm and induced myopia, reduced visual acuity in low light (due to miosis), decreased corneal sensitivity, point keratitis, allergic blepharoconjunctivitis; very rarely - diplopia and ptosis.
Several cases of retinal detachment, iris stiffness or cyst formation in the iris have been noted in connection with the use of miotic means. With prolonged use of pilocarpine, a reversible clouding of the lens was observed.
Systemic reactions: nausea, diarrhea, increased sweating, increased salivation, decrease in blood pressure, exacerbation of bronchial asthma, heart failure, bradycardia, arrhythmia, temporal and supra-orbital headaches, skin rash.
Timolol penetrates the BBB and has an impact on the central nervous system.
In all patients with heart failure, timolol can cause asthenic syndrome, nausea, dizziness, anxiety, hallucinations, headache, and depression.
Very rarely nasal congestion was noted.
Contraindications
WITH caution the drug should be prescribed for heart failure, cerebrovascular disorders, diabetes mellitus, hypoglycemia, retinal detachment, myopia, thyrotoxicosis, before surgery under general anesthesia.
Drug interactions
When using Fotil (which includes timolol), simultaneously with beta-blockers for oral administration, the pharmacological effect of beta-blockers is enhanced.
With simultaneous use of the drug Fotil with calcium channel blockers such as verapamil, AV conduction disturbances, development of left ventricular failure, arterial hypotension are possible.
With simultaneous use of Fotila with drugs that promote the release of catecholamines (for example, with reserpine), in isolated cases hypotension (including rotostatic hypotension), bradycardia, dizziness were observed.
Pregnancy and Lactation
To date, no adequate and well controlled studies have been conducted in pregnant women.
Use of Fotil during pregnancy and lactation is possible only when the intended benefit to the mother outweighs the potential risk to the fetus.
In experimental studies, no negative effect of timolol on fertility was detected.
Currently, there is no evidence that during the treatment of glaucoma in humans, pilocarpine has a teratogenic effect.
Special instructions
The drug is prescribed to patients who can not compensate for increased intraocular pressure using monotherapy in almost all forms of glaucoma.
Caution should be prescribed the drug in the following cases:
- Patients with cerebrovascular disorders.
- When hypoglycemia.
- Before surgery under anesthesia.
Caution must be exercised in the appointment of the drug to patients receiving beta-blockers inside.
With prolonged use of the drug in patients with glaucoma may develop resistance to the active components of the drug. However, to the combined eye drops, the degree of development of tolerance is less pronounced than to monocomponent antiglaucoma preparations.
Evaluation of the effectiveness of the drug should be approximately 4 weeks after the start of treatment. Measurement of intraocular pressure should be carried out at different times of the day.
Due to the fact that the product contains a preservative, patients who wear soft contact lenses should remove them before using the drops. It is recommended to wait 15 minutes before reinserting contact lenses.
During the period of use of the drug dark adaptation may worsen. The patient should be warned about the danger of movement in the dark.
Use in Pediatrics
Clinical trials of the safety and efficacy of Fotil in children have not been conducted.
The results of experimental studies
In studies conducted on laboratory animals, no mutagenic action of timolol was detected.
Currently, there is no evidence that during the treatment of glaucoma in humans, pilocarpine has a mutagenic effect. However, in experimental studies revealed signs of mutagenicity of pilocarpine.
Influence on ability to drive motor transport and control mechanisms
Drivers of motor vehicles should be careful when driving in low light conditions, because The drug may interfere with dark adaptation.
Overdosage
- Symptoms: bradycardia, arterial hypotension, bronchospasm, acute heart failure.
- Treatment: conduct symptomatic therapy. Atropine can be used as an antidote to pilocarpine. The purpose of isoprenaline for severe bradycardia, bronchospasm is shown; dobutamine - for hypotension; cardiac glycosides, diuretic drugs - in the event of acute heart failure.
- Active ingredient: Pilocarpine
Studies and clinical trials of Pilocarpine (Click to expand)
- Disinfection of the East-Radcliffe ventilator : A bacteriological study of a modified picloxydine technique
- Loss of NADPH diaphorase-positive neurons in the hippocampal formation of chronic pilocarpine-epileptic rats
- Cell damage and neurogenesis in the dentate granule cell layer of adult rats after pilocarpine- or kainate-induced status epilepticus
- Urticaria associated with the pilocarpine iontophoresis sweat test
- Protective effect of Withania somnifera root extract on electrographic activity in a lithium-pilocarpine model of status epilepticus
- Effectiveness of pilocarpine in postradiation xerostomia
- Use of pilocarpine during head and neck radiation therapy to reduce xerostomia and salivary dysfunction
- The maturation of the rabbit fetal lung following maternal administration of pilocarpine
- Reduced cell proliferation in fetal lung after maternal administration of pilocarpine. A scintillation autoradiographic study
- Pilocarpine-loaded poly(DL-lactic-co-glycolic acid) nanoparticles as potential candidates for controlled drug delivery with enhanced ocular pharmacological response
- Ultrastructural stereologic analysis of fetal rabbit type II alveolar epithelial cells following maternal pilocarpine treatment or fasting
- Secretory process in Brunner's glands during recovery from stimulation with a single dose of pilocarpine
- Cell distribution in tracheal surface epithelium and the effects of long-term pilocarpine and atropine administration
- Proteomic study of salivary peptides and proteins in patients with Sjögren's syndrome before and after pilocarpine treatment
- Age-related differences in ophthalmic drug disposition I. Effect of size on the intraocular tissue distribution of pilocarpine in albino rabbits
- Age-related differences in ophthalmic drug disposition II: Drug-protein interactions of pilocarpine and chloramphenicol
- ChemInform Abstract: Palladium-Catalyzed Intramolecular Alkyne-α,β-Unsaturated Carbonyl Coupling. A Formal Synthesis of (+)-Pilocarpine.
- Highly Enantioselective Syntheses of Functionalized α-Methylene-γ-butyrolactones via Rh(I)-Catalyzed Intramolecular Alder Ene Reaction: Application to Formal Synthesis of (+)-Pilocarpine.
- Synthesis of Chiral Pilocarpine Analogues (II), (III) via a C-8 Ketone Intermediate (I).
- Loss of interneurons innervating pyramidal cell dendrites and axon initial segments in the CA1 region of the hippocampus following pilocarpine-induced seizures
- Cellular and network properties of the subiculum in the pilocarpine model of temporal lobe epilepsy
- Hippocampal granule cell activity and c-Fos expression during spontaneous seizures in awake, chronically epileptic, pilocarpine-treated rats: Implications for hippocampal epileptogenesis
- Changes in vesicular transporters for γ-aminobutyric acid and glutamate reveal vulnerability and reorganization of hippocampal neurons following pilocarpine-induced seizures
- Region-specific alterations in astroglial TWIK-related acid-sensitive K+-1 channel immunoreactivity in the rat hippocampal complex following pilocarpine-induced status epilepticus
- Region-specific alterations in astroglial TWIK-related acid-sensitive K+-1 channel immunoreactivity in the rat hippocampal complex following pilocarpine-induced status epilepticus
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