SAR of cholinolytic agents: Solanaceous alkaloids and analogues: Atropine sulphate, Hyoscyamine sulphate, Scopolamine hydrobromide, Homatropine hydrobromide, Ipratropium bromide : Pharmaguideline -->

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SAR of cholinolytic agents: Solanaceous alkaloids and analogues: Atropine sulphate, Hyoscyamine sulphate, Scopolamine hydrobromide, Homatropine hydrobromide, Ipratropium bromide

Solanaceous alkaloid ad analogues as primarily found in henbane (Hyoscyamus niger), jimson weed (Datura stramonium) and deadly nightshade.
Solanaceous alkaloid ad analogues as primarily found in henbane (Hyoscyamus niger), jimson weed (Datura stramonium) and deadly nightshade (Atropa belladonna).

Examples: Atropine sulphate, Hyoscyamine sulphate, Scopolamine hydrobromide, Homatropine hydrobromide, Ipratropium bromide

Atropine sulphate

  • It is used in corneal inflammation and iritis
  • It is used in the treatment of arrhythmias by increasing heart rate
  • It produces mydriatic effect as it causes pupil dilation
  • It prevents the muscarinic effects of ACh accumulation; hence, used as an antidote in organophosphate poisoning
  • It is administered before general anaesthesia by decreasing nasal and oral secretions
SAR-
R1 or R2 should be heterocyclic or carbocyclic.
The R3 group can be hydrogen, hydroxyl, hydroxymethyl or amide.
It comes from something stronger than X as an ester.
The X may also be oxygenated or completely absent.
Area N can be quaternary ammonium salt or tertiary amine or both with different alkyl groups.
The maximum power obtained when the distance between the flexible carbon ring is 2 units of carbon.

Hyoscyamine sulphate

  • Hyoscyamine sulphate is the levorotatory form of atropine
  • It is used as an anticholinergic agent
  • It is used to treat many intestinal or stomach problems such as IBD and cramps
SAR-
Hyoscyamine is an alkaloid of tropane and a levo-isomer of atropine. It is usually extracted from the family plants Solanaceae or nightshade. Research on the action of hyoscyamine in publications published since 1826. Hyoscyamine is used in a variety of treatments and therapies due to its antimuscarinic properties.

Although hyoscyamine is marketed in the United States, it is not approved by the FDA.

Scopolamine hydrobromide

  • Scopolamine hydrobromide is also known as hyoscine. Belladonna alkaloids produce the same effects as atropine.
  • Its duration of action is shorter than that of atropine.
  • It is used in the treatment of motion sickness as it suppresses vestibular disturbances by inhibiting cholinergic activity. The medication can be taken orally or transdermally. The transdermal patch is generally placed behind the ear, over the mastoid process
  • It is used in the post-operative nausea and vomiting
  • Like atropine, it is given before surgery to reduce salivary secretions
  • Scopolamine causes dryness of mouth and sedation
SAR-
Scopolamine disrupts the transmission of nerve impulses by Ach to the parasympathetic nervous system. It works especially well in the laundry area.

Homatropine hydrobromide

  • It is a semisynthetic atropine derivative
  • It is not as potent as atropine with a duration of action of 1 to 3 days
  • It is the anticholinergic agent of choice before eye examination and post-operative eye surgeries
  • It inhibits the muscarinic action of acetylcholine
  • It causes the widening of the pupil
SAR-
Homatropin blocks muscarinic receptors and cholinergic signaling pathways.
It prevents responses from the iris sphincture muscle and causes the reader to not respond to light when opening or mydriasis.
Homatropin also inhibits ciliary immune function in cholinergic stimulation.

Ipratropium bromide

  • Ipratropium bromide is a quaternary compound
  • It is given by inhalational route of administration
  • It has selective action on bronchial smooth muscle and produces bronchodilation. It promotes muscle relaxation to facilitate proper breathing
  • Chronic obstructive pulmonary diseases such as COPD can cause shortness of breath and wheezing symptoms that can be controlled by ipatropium bromide.
  • Despite these functions, it is not involved in mucociliary clearance.
  • Emphysema and bronchitis are treated with it.
  • The major side effect of this drug is dryness of the mouth
SAR-
i. The drug blocks the parasympathetic nervous system in the air.
ii. Ipratropium stops acetylcholine activity in smooh muscles and prevents access to free airways.
iii. This leads to bronchodilation and a few secretions.
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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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