Synthetic cholinergic blocking agents: Methantheline bromide, Propantheline bromide, Benztropine mesylate, Orphenadrine citrate, Biperidine hydrochloride : Pharmaguideline -->

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Synthetic cholinergic blocking agents: Methantheline bromide, Propantheline bromide, Benztropine mesylate, Orphenadrine citrate, Biperidine hydrochloride

Methantheline bromide is a synthetic cholinergic blocking agent that acts as a competitive antagonist of acetylcholine at muscarinic receptors.

Methantheline bromide

Methantheline bromide is a synthetic cholinergic blocking agent that acts as a competitive antagonist of acetylcholine at muscarinic receptors.

Methantheline bromide can also be used as a premedication to reduce the secretory activity of the salivary and bronchial glands before surgery.
  • Methantheline bromide is available in tablets or injections. The recommended dose is 10-20 mg thrice a day. The injectable form is given intramuscularly or intravenously.
  • Patients with cardiovascular disease, renal impairment, and GI obstruction should be cautious while taking this medication.
  • Methantheline bromide can cause dry mouth, blurred vision, constipation, and urinary retention. It can also cause hypotension and arrhythmias.
SAR of Methantheline bromide
Methantheline bromide is a synthetic compound that acts by blocking acetylcholine receptors in the central and peripheral nervous systems. This mechanism of action has shown potential for treating a variety of neurological disorders, including Alzheimer's disease, Parkinson's disease, and epilepsy.

There is a great deal of research ongoing to explore the full therapeutic potential of methantheline bromide. Some promising early results suggest that this compound may one day be used as a treatment option for these debilitating disorders. However, more robust clinical trials are needed to further evaluate its safety and effectiveness in patients.

The structure-activity relationship (SAR) of methantheline bromide has been extensively studied, and researchers have identified several key structural features that are critical to its activity. These include the presence of a benzyl side chain and an oxygen atom at position 4 of the Pyrrolidine ring, as well as a substitution at positions 2 and 6 of the ring.

Propantheline bromide

Propantheline bromide is used for the symptomatic relief of postoperative urinary retention and for neurogenic bladder dysfunction.
  • Propantheline bromide (PB) is a medication used to relieve muscle spasms of the gastrointestinal tract, bladder, and ureters.
  • PB belongs to a class of drugs called anticholinergics/antispasmodics. This medication works by relaxing the smooth muscle in the gastrointestinal tract, bladder, and ureters.
  • The medication is accessible in tablet as well as liquid form. The usual adult dose is 10-20 mg 3-4 times daily.
SAR of Propantheline bromide:
The SAR of propantheline bromide is similar to that of methantheline bromide. Both compounds have a benzyl side chain and an oxygen atom at position 4 of the Pyrrolidine ring, which is critical for their activity. However, propantheline bromide has a weaker affinity for acetylcholine receptors compared to methantheline bromide, due to the presence of an extra methyl group at position 3 of the Pyrrolidine ring.

Despite some promising early results, more research is needed to fully understand the mechanisms of action and therapeutic potential of these synthetic cholinergic blocking agents. There may also be other compounds with similar structures that could be developed as more potent and specific treatments for neurological disorders.

Benztropine mesylate


Uses:
It is used in the treatment of Parkinson's disease, as it blocks the excessive activation of dopamine receptors caused by the disease.

Side effects of Benztropine:
  • Constipation
  • Dizziness
  • Dry mouth
  • Blurred vision
  • Hallucinations
  • Irregular heartbeat
  • Seizures
SAR of Benztropine mesylate:
Like methantheline bromide and propantheline bromide, benztropine mesylate is a synthetic cholinergic blocking agent that acts by inhibiting acetylcholine receptors in the central and peripheral nervous systems. However, this compound is distinct from other cholinergic blockers due to its quaternary amine structure. This feature gives benztropine mesylate a much higher affinity for acetylcholine receptors, making it a more potent and effective treatment for neurological disorders.

Orphenadrine citrate




  • Orphenadrine citrate is usually taken two or three times a day.
  • The injectable form of this medication may be given into a vein or muscle as directed by your doctor.
If you are taking the tablet form of this medication, take it with food or milk to decrease stomach upset. If you are using the injectable form of this medication, do not mix it with other medications in the same infusion (drip).

SAR of Orphenadrine citrate:
Orphenadrine citrate is another synthetic cholinergic blocking agent that has a quaternary amine structure. This gives it a higher affinity for acetylcholine receptors and makes it a more potent and effective treatment for neurological disorders. However, orphenadrine citrate also has some additional features that make it unique from other cholinergic blockers. These include the presence of a tertiary amine group and an oxygen atom at position 2 of the Pyrrolidine ring. These features give orphenadrine citrate greater stability and a longer duration of action compared to other cholinergic blocking agents.

Biperidine hydrochloride

Biperiden hydrochloride is a synthetic cholinergic blocking agent.
  • It is used to treat various conditions that result from overactivity of the parasympathetic nervous system, such as abdominal cramps, diarrhea, and vomiting. It can be used to soothe motion sickness.
  • Biperiden hydrochloride works by preventing the action of acetylcholine, a neurotransmitter that is responsible for these conditions.
  • The drug is accessible in the form of tablets and injections. It should be taken orally, usually three or four times a day. The injection should be given intramuscularly or intravenously, depending on the condition being treated.
  • Biperiden hydrochloride should not be used by people who are allergic to it or to any other ingredient in the medication. It should also be used with caution in people with certain medical conditions, such as asthma, COPD, heart disease, kidney disease, or liver disease.
SAR of Biperidine hydrochloride:
The SAR value for Biperidine hydrochloride is quite low, meaning that its interactions with the cellular environment are not very strong. According to Robert et al.'s study, this could make it a potentially safe drug with low toxicity. However, further studies will be needed to confirm this.

In summary, the SAR value for Biperidine hydrochloride is a reasonable indicator of its potential toxicity. Further studies are needed to confirm this, but the evidence so far suggests that it is a safe drug with low toxicity.
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Ankur Choudhary is India's first professional pharmaceutical blogger, author and founder of Pharmaceutical Guidelines, a widely-read pharmaceutical blog since 2008. Sign-up for the free email updates for your daily dose of pharmaceutical tips.
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