الحلقة 7 من كورس كلنيكال فارما (ANS)

Atropine Substitutes

EYE

Homatropine

(Isopto® Homatropine)

Cyclopentolate

(Cicloplejico®)

Tropicamide

(Mydriacyl®)

-Cyclopentolate and Tropicamide used for mydriasis and cycloplegia (before eye

examinations).

Phenylephrine (or similar a-adrenergic drugs) are preferred for mydriasis if cycloplegia is

not required.

- Cyclopentolate + Phenylephrine (Cyclophrine)

* More preferred for mydriasis with less cycloplegia effect.

- Homatropine more preferred in uveitis and iritis.

GIT

Hyoscine (or Scopolamine) N-Butylbromide (Buscopan®)

-Hyoscine butylbromide, most popular antispasmodic drug, relief spasms in the gastro-

intestinal (GI) or genito-urinary (GU) tract.

Tiemonium (Viscéralgine®)

-Tiemonium , antispasmodic drug relief GI/GU tract spasms.

Dicyclomine or Dicycloverine (Bentyl®)

Dicyclomine or Dicycloverine , used to reduce the GI cramping especially colon spasm

{irritable bowel syndrome (IBS)}

Propantheline (Pro-Banthine®) Oxyphenonium (Anil®)

- Oxyphenonium and Propantheline are antispasmodic drugs.

- Also used in stomach ulcers in combination with other drugs.

Glycopyrrolate or Glycopyrronium (Robinul®)

Glycopyrrolate ,Anti-secretory drug.

-Used in anesthesia, as a preoperative medication (reduce salivary, trachea, and

pharyngeal secretions, as well as decreasing the acidity of gastric secretion).

Clidinium (Librax®)

- Clidinium , used for reduce cramping and gastric acidity.

- It is commonly prescribed in combination with chlordiazepoxide (benzodiazepine

derivative) for treatment IBS. (Librax®).

Pirenzepine (Gastrozepin®) Telenzepine

- Used (rarely) in peptic ulcer with other drugs reduces gastric acid secretion (selective M1

receptor) (see GIT chapter).

Respiratory

System

Ipratropium (Atrovent®) Tiotropium (Spiriva®)

Ipratropium and Tiotropiumt, are approved as bronchodilators for maintenance treatment

of bronchospasm associated with chronic obstructive pulmonary disease (COPD).

- Ipratropium is also used in the acute management of bronchospasm in asthma.

- Both agents are delivered via inhalation Because of their +ve charges (quaternary

ammonium), these drugs do not enter the systemic circulation or the CNS.

- Duration of action : Tiotropium (24 hours; once daily) longer in duration than

Ipratropium (4 hours; up to four times daily).

Atropine

Substitutes

Urinary

Bladder

Oxybutynin (Uripan®) Tolterodine (Detrusitol®)

Darifenacin (Enablex®) Fesoterodine (Toviaz®)

Solifenacin (Vesicare®) Flavoxate (Genurin S.F®)

Trospium (Spasmolyt®) Propiverine (Mictonorm®)

Emepronium (Cetiprin®)

- All of these drugs used to reduces muscle spasms of the bladder and urinary tract.

- All of these drugs used to treat symptoms of overactive bladder (OAB), such as frequent or urgent

urination, incontinence, and increased night-time urination.

- All of these drugs contraindicated in: urinary retention, gastric retention and closed-angle

glaucoma.

-Oxybutynin & Tolterodine are most common used. Oxybutynin is available as a

transdermal system (topical patch).

- Darifenacin is indicated for the treatment of OAB with symptoms of urge urinary

incontinence in adults.

- Fesoterodine is a prodrug. It is broken down into its active metabolite, 5-hydroxymethyl

Tolterodine.

- Solifenacin is metabolized in the liver by the cytochrome-P450 (CYP3A4) drug interaction;

with LME inhibitors. May also prolong the QT interval (type of arrhythmia)

Contraindicated in patient with long QT interval.

- Flavoxate is indicated for symptomatic relief of interstitial cystitis, dysuria, urgency,

nocturia, supra-pubic pain, frequency and incontinence as may occur in cystitis,

prostatitis, urethritis, urethrocystitis/urethrotrigonitis.

- Trospium should be taken at least one hour before meals or given on an empty stomach.

- Emepronium may cause ulceration of esophagus, so it should be taken in orthostatic

position with sufficient amounts of liquids.

CNS

Benztropine (Cogintol®) Biperiden (Akineton®)

Trihexyphenidyl (parkinol")

Benztropine ,Biperiden and Trihexyphenidyl are used in treatment of Parkinson's disease in

combination with other drugs. (see CNS chapter).

Orphenadrine (Norflex®)

- Orphenadrine is a skeletal muscle relaxant, relief pain due to spasm of skeletal muscle. It works by

blocking nerve impulses that are sent to brain.

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