And Sodium Phosphate
And Sodium Phosphate Uses, Dosage, Side Effects, Food Interaction and all others data.
Hyoscyamine is a tropane alkaloid and the levo-isomer of atropine. It is commonly extracted from plants in the Solanaceae or nightshade family. Research into the action of hyoscyamine in published literature dates back to 1826. Hyoscyamine is used for a wide variety of treatments and therapeutics due to its antimuscarinic properties.
Although hyoscyamine is marketed in the United States, it is not FDA approved.
Hyoscyamine is not FDA approved, and so it has not official indications. However, it is used as an antimuscarinic agent in a number of treatments and therapies. Hyoscyamine has a short duration of action as it may need to be given multiple times per day. Patients should be counselled regarding the risks and signs of anticholinergic toxicity.
Methenamine is a heterocyclic organic compound with a cage-like structure similar to adamantane. In salt form it is used for the treatment of urinary tract infection (Example: methenamine hippurate which is the hippuric acid salt of methenamine).
Ingestion of a 1-gram dose of methenamine hippurate produces antibacterial activity in the urine within 1/2 hour. Administration of 1 g twice daily produces continuous antibacterial activity in the urine.
Methylene blue is an oxidation-reduction agent. The intravenous form of methylene blue is approved by the FDA for the treatment of pediatric and adult patients with acquired methemoglobinemia. Historically, it has been widely used in Africa to treat malaria, but now it disappeared when chloroquine (CQ) and other drugs entered the market. Its use as an urinary tract antiseptic has also been investigated.
Methylthioninium chloride (INN, or methylene blue, proposed trade name Rember) is an investigational drug being developed by the University of Aberdeen and TauRx Therapeutics that has been shown in early clinical trials to be an inhibitor of Tau protein aggregation. The drug is of potential interest for the treatment of patients with Alzheimer's disease.
Phenyl salicylate is a 2-hydroxybenzoic acid phenyl ester. It is utilized in some manufacturing processes of polymers, lacquers, adhesives, waxes, as well as polishes. It is an active ingredient in some pharmaceutical products as a mild analgesic for pain relief by releasing salicylate (found in Aspirin ). Phenyl salicylate may also be found in some antiseptic agents . It is synthesized by heating salicylic acid with phenol , .
Phenyl salicylate is used as a food additive in the USA .
This compound belongs to the class of organic compounds known as depsides and depsidones. These are polycyclic compounds that is either a polyphenolic compound composed of two or more monocyclic aromatic units linked by an ester bond (depside), or a compound containing the depsidone structure (depsidone) .
| Trade Name | And Sodium Phosphate |
| Generic | Hyoscyamine + methenamine + methylene blue + phenyl salicylate + sodium biphosphate |
| Type | Oral |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Hyoscyamine is an anticholinergic indicated to treat functional gastrointestinal disorders, biliary and renal colic, and acute rhinitis.
As a drug that is not FDA approved, hyscyamine has no official indications. Intravenous hysocyamine has been used to reduce gastric motility, reduce pancreatic pain and secretions, to facilitate imaging of the gastrointestinal tract, treat anticholinesterase toxicity, treat certain cases of partial heart block, improve visualization of the kidneys, and for symptomatic relief of biliary and renal colic. Intravenous hyoscyamine is also used pre-operatively to reduce secretions of the mouth and respiratory tract to facilitate intubation. Oral hyoscyamine is used to treat functional intestinal disorders, for symptomatic relief of biliary and renal colic, and symptomatic relief of acute rhinitis.
Methenamine is a urinary tract antiseptic and antibacterial drug used for the prophylaxis and treatment of frequently recurring urinary tract infections requiring a long-term therapy.
For prophylactic or suppressive treatment of frequently recurring urinary tract infections when long-term therapy is considered necessary. This drug is not used to treat infection and should only be used after appropriate eradication of infection with antimicrobial agents.
Methylene blue is an oxidation-reduction agent used for the treatment of pediatric and adult patients with acquired methemoglobinemia.
Indicated for the treatment of pediatric and adult patients with acquired methemoglobinemia.
Other clinical applications of methylene blue include improvement of hypotension associated with various clinical states, an antiseptic in urinary tract infections, treatment of hypoxia and hyperdynamic circulation in cirrhosis of liver and severe hepatopulmonary syndrome, and treatment of ifofosamide induced neurotoxicity.
Pain and fever .
And Sodium Phosphate is also used to associated treatment for these conditions: Biliary Colic, Colic, Cystitis, Diverticulitis, Heart Block, Irritable Bowel Syndrome (IBS), Neurogenic Bladder Dysfunction, Neurogenic Bowel Dysfunction, Pancreatitis, Parkinsonism, Peptic Ulcer, Poisoning caused by anticholinesterases, Pylorospasm, Renal Colic, Spastic bladder, Tracheo-bronchial secretion excess, Acute Enterocolitis, Acute Rhinitis, Gastric secretions, Mild Dysentery, Pharyngeal secretions, Salivary secretions, Spastic colitisUrinary Tract InfectionCystitis, Methaemoglobinaemia, Nephritis, Urethritis, Urinary tract inflammation, Diuresis
How And Sodium Phosphate works
Hyoscyamine competitively and non-selectively antagonises muscarinic receptors in the smooth muscle, cardiac muscle, sino-atrial node, atrioventricular node, exocrine nodes, gastrointestinal tract, and respiratory tract. Antagonism of muscarinic M1, M4, and M5 receptors in the central nervous system lead to cognitive impairment; antagonism of M2 in the sinoatrial and atrioventricular nodes leads to bradycardia and lowers contractility; and antagonism of M3 in smooth muscle results in reduced peristalsis, bladder contraction, salivary secretions, gastric secretions, bronchial secretions, sweating, increased bronchodilation, mydriasis, and cycloplegia.
Methenamine does not have antibacterial properties in an alkaline environment (pH≥6); however, in a more acidic environment (pH<6), methenamine is hydrolyzed to formaldehyde. (1) Formaldehyde is considered to be highly bactericidal. (1) Formaldehyde has nonspecific antibacterial activity and works by denaturing proteins and nucleic acid of bacteria. (1) Certain bacteria such as Proteus sp. can alkalize urine, inhibiting the beneficial activity of formaldehyde. (1) The key role of the salt component of the drug, for example hippuric acid, is to maintain the acidic state of the urine. (1)
- Main mechanism of action involves inhibition of nitric oxide synthase and guanylate cyclase.
- In Alzheimers Disease: a mechanistic study found that methylene blue oxidizes cysteine sulfhydryl groups on tau to keep tau monomeric. One preclinical treatment study in tauopathy mice reported anti-inflammatory or neuroprotective effects mediated by the Nrf2/antioxidant response element (ARE); another reported insoluble tau reduction and a learning and memory benefit when given early.
- In Methemoglobinemia: Methylene Blue acts by reacting within RBC to form leukomethylene blue, which is a reducing agent of oxidized hemoglobin converting the ferric ion (fe+++) back to its oxygen-carrying ferrous state(fe++).
- As antimalarial agent: Methylene Blue, a specific inhibitor of P.falciparum glutathione reductase has the potential to reverse CQ resistance and it prevents the polymerization of haem into haemozoin similar to 4-amino-quinoline antimalarials.
- For ifosfamide induced neurotoxicity: Methylene blue functions as an alternate electron acceptor. It acts to reverse the NADH inhibition caused by gluconeogenesis in the liver while blocking the transformation of chloroethylamine into chloroacetaldehyde. In addition, it inhibits various amine oxidase activities, which also prevents the formation of chloroacetaldehyde.
Inhibits the activity of the enzyme known as cyclooxygenase (COX) which causes the formation of prostaglandins, substances which cause inflammation, swelling, pain, and fever . For more information, refer to the drug entry Aspirin.
Toxicity
Patients experiencing an overdose may present with headache, nausea, vomiting, dizziness, dry mouth, difficulty in swallowing, dilated pupils, blurred vision, urinary retention, hot dry and flushed skin, tachycardia, hypertension, hypotension, respiratory depression, CNS stimulation, fever, ataxia, excitation, lethargy, stupor, coma, and paralysis. Patients should be treated with symptomatic and supportive therapy which may include emesis, gastric lavage, activated charcoal, artificial respiration, or intravenous physostigmine. Dialysis is expected to remove hyoscyamine sulfate from circulation.
Less than 3.5% of patients treated with this drug will experience minor adverse events such as upset stomach, dysuria, nausea, and rash.
LD50 = 1180 mg/kg ( Rat ).
Oral LD50 in the rat is 3000 mg/kg
Adverse effects can be divided into several categories , :
Eyes: irritation
Skin: skin irritation
Cardiovascular: rapid pulse, flushing
Central Nervous System —blurred vision, dizziness
Respiratory —shortness of breath or troubled breathing , irritation of respiratory system
Genitourinary —difficult micturition, acute urinary retention
Gastrointestinal —dry mouth, nausea/vomiting
Overdosage may be managed by inducing emesis or gastric lavage. Slow intravenous administration of physostigmine in doses of 1 to 4 mg (0.5 to 1 mg in children) repeated as needed in 1-2 h to relieve severe antimuscarinic symptoms. Administration of small doses of diazepam to control excitement and seizures may be warranted. Artificial respiration with oxygen can be used if needed for respiratory depression. Adequate hydration is important, as well as symptomatic treatment, provided as necessary .
Volume of Distribution
10 mg/kg (in rats).
Steady-state plasma salicylate concentrations increase more than proportionally with increasing dosages; the time required to reach steady state increases with increasing daily dose. Dosage intervals of 8-12 h are sufficient to maintain plasma salicylate concentrations in the normal therapeutic anti-inflammatory concentration range .
Elimination Route
Hyoscyamine is completely absorbed by sublingual and oral routes, though exact data regarding the Cmax, Tmax, and AUC are not readily available.
After oral administration, rapid absorption of methenamine occurs. (1)
Rapidly absorbed. Refer to Aspirin for detailed salicylate absorption information.
Half Life
The half life of hyoscyamine is 3.5 hours.
Elimination half-life = 3-4 hours assuming normal renal function. (1)
5–6.5 hours (after IV dose).
Mean half-life of 1.1 h .
Clearance
70-90% of a single oral dose of methenamine is excreted unchanged in the urine within 24 hours. (1)
3.0 ± 0.7 L/min.
Please refer to Aspirin for more information.
Elimination Route
The majority of hyoscyamine is eliminated in the urine as the unmetabolized parent compound.
Methenamine is primarily eliminated via the kidneys. (1)
Excreted in urine and bile. About 75% of an oral dose excreted in urine, primarily as stabilized colorless leukomethylene blue.
Please refer to Aspirin for the route of elimination.
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