Cuvposa vs Robinul

Published 2016-08-12 18:13:00 drugs

Cuvposa vs Robinul

Indications: Sialorrhea (Drooling)

Sialorrhea or drooling resulting in saliva beyond the lip is common in babies and infants. It resolves between 15 months and 18 months during normal development. But drooling up to 3 years of age is not uncommon.

In children with neurological disorders (e.g., cerebral palsy) severe constant drooling is a recurring issue.

Sialorrhea can also be a problem in adults with Parkinson’s disease or that have had a stroke. 1

Drooling can be caused by multiple dysfunctions including hypersecretion of saliva; anatomical abnormalities; and, sensory, motor and neuromuscular dysfunctions.

Hypersecretion is caused by oral inflammation such as teething and tooth decay. Sensory dysfunctions may prevent the recognition of the need to swallow results in drooling.

Anatomical abnormalities, such as an enlarged tongue or teeth misalignment may also result in excessive drooling. This is most common in children with neurological disorders is neuromuscular dysfunction. Lack of facial and/or oral muscle control (specifically tongue control) is plays a big role in sialorrhea among these children. 2

Common Side Effect of Chronic Drooling

  • skin breakdown
  • chapped lips
  • dehydration
  • and unpleasant odor
  • as well as social complications, like embarrassment and isolation. 3

How to Prevent Excessive Drooling

  • changes in diet and/or habit
  • oral-motor exercises, and /or intra-oral training devices
  • In more severe cases, surgery, radiation or treatment with anticholinergic agents that reduce saliva secretion may be needed.

Acetylcholine (Ach)

Anticholinergics block a chemical called acetylcholine (Ach) from stimulating muscle activity.

The brain prompts muscles (in this case the muscles around the salivary ducts) to contract via acetylcholine release from nerve cells. Ach binds to Ach receptors on the muscle which stimulates it to contract. Anticholinergics bind to Ach receptors without activating them to prevent Ach binding and muscle contraction. These drugs are used to treat several diseases such as:

  • asthma
  • incontinence
  • gastrointestinal cramps and muscle spasm by preventing involuntary muscle movements in these conditions.

In the case of salivation, anticholinergics block signaling from the parasympathetic nerve, which stimulates glands involved in salivation, in order to reduce salivation rate. 4

Common Treatment for Drooling

The best therapies include: - botulinum toxin A - scopolamine - and glycopyrrolate

While botulinum toxin A has few side effects and is effective for several months, its effects eventually wear off and thus it requires repeated injections. Treatment is also very expensive compared to the other treatments.

Scopolamine is a patch that is applied to the skin every day. While cheaper than botulinum toxin A, it is associated with many more side effects such as severe itching near the patch, an inability to urinate and dizziness. Glycopyrrolate, while having similar side effects to the patch, is much cheaper and is very effective at reducing drooling. 5

Glycopyrrolate (Robinul)

Glycopyrrolate (Brand name: Robinul) was approved by the US Food and Drug Administration (FDA) in August 1961. While not indicated for treating drooling in children with neurological disorders, it is typically used to reduce saliva secretion. Robinul is indicated for use as a preoperative anticholinergic to reduce oral and airway secretions. It is also indicated to treat peptic ulcer. 6

Dosage of Robinul

Glycoprryolate is a white, odorless cystralline powder that is soluble in water and alcohol. Rubinol consists of glycopyrrolate dissolved in water. Alcohol is added as a preservative. The resulting clear, colorless, sterile liquid is administered intramuscularly or intravenously.

For preanesthetic medication, Robinul is administered at a concentration of 0.004mg/kg by intramuscular injection 30min to an hour before anesthesia is induced in adults and children. Rubinol is effective within a minute after administration. Its effects are experienced within 15 to 30 minutes, with peak effects occurring at 30 to 45 minutes. It’s saliva decreasing effects last for up to 7 hours. As mentioned previously, Rubinol has side effects many side effects.

Common Side Effects of Robinul

  • drowsiness
  • dizziness
  • weakness
  • blurred vision
  • dry eyes
  • dry mouth
  • constipation
  • and abdominal bloating. 7

Although effective at reducing salivation in children, intramuscular and intravenous injection is not the most child friendly method of administering treatment to children. Thus, there was a need for an easier and less painful method of administration. The solution was provided several decades later on July 28, 2010, when Glycopyrrolate oral solution (Brand name: Cuvposa) became the first drug approved by the FDA to treat drooling in children with neurological conditions. 8

Glycopyrrolate (Cuvposa)

Dosage of Cuvposa

Cuvposa is available in 5mL clear cherry-flavored solutions (containing 1mg of glycopyrrolate) to be administered orally in 16 ounce bottles. Cuvposa is initially administered in 0.02mg/kg doses orally three times a day.

Since absorption is significantly lower when administered with a high fat meal, it also needs to be administered 1 to 2 hours after meals. Dosage is adjusted every 5 to 7 days until the optimal dosage is determined with the least severe side effects without exceeding 0.1mg/kg three times a day.

Cuvposa does have some drawbacks, however. Compared to intravenous and intramuscular injection, Cuvposa takes longer to take effect. However, Cuvposa has a slightly longer half-life (3.1 hours compared to 3 hours) and can be detected in plasma for up to 12 hours. This has translated into a longer duration of salivation reduction. Another shortcoming is that it also needs to be administered several times a day.

Common Side Effects of Cuvposa

Cuvposa is also associated with side effects. - dray mouth - vomiting - constipation - flushing - and nasal congestion. 9

Wrapping It Up

Excessive salivary secretion in children with neurological disorders is a major problem.

The more severe cases are treated with anticholinergic agents that reduce salivation rate by blocking stimulation of muscles involved in salivation by the parasympathetic nerve.

Until recently, the best anticholinergic was Robinul, a form of glycopyrrolate that is injected intravenously or intramuscularly.

In the last few years, however, a more child-friendly oral formulation called Cuvposa was developed. While the oral form is similar to the injectable form in efficacy, it has some drawbacks including repeated daily treatments, and a delay in when the effects are felt by the patient. Still, this new therapy has provided a novel, easy and less painful method of treating drooling in children with neurological diseases. 10

References

  1. Lakraj AA, Moghimi N, Jabbari B. Sialorrhea: anatomy, pathophysiology and treatment with emphasis on the role of botulinum toxins. Toxins (Basel). 2013;5(5):1010-31. 

  2. Leung AK, Kao CP. Drooling in children. Paediatr Child Health. 1999;4(6):406-11. 

  3. Walshe M, Smith M, Pennington L. Interventions for drooling in children with cerebral palsy. Cochrane Database Syst Rev. 2012;11:CD008624. 

  4. Available at: http://www.ncbi.nlm.nih.gov/books/NBK217767/. Accessed August 5, 2016. 

  5. Sławek J, Madaliński MH, Maciag-tymecka I, Duzyński W. [Frequency of side effects after botulinum toxin A injections in neurology, rehabilitation and gastroenterology]. Pol Merkur Lekarski. 2005;18(105):298-302. 

  6. Available at: http://www.ncbi.nlm.nih.gov/pubmedhealth/PMHT0000827/. Accessed August 5, 2016. 

  7. Available at: http://www.ncbi.nlm.nih.gov/pubmedhealth/PMHT0010492/. Accessed August 5, 2016. 

  8. Zeller RS, Davidson J, Lee HM, Cavanaugh PF. Safety and efficacy of glycopyrrolate oral solution for management of pathologic drooling in pediatric patients with cerebral palsy and other neurologic conditions. Ther Clin Risk Manag. 2012;8:25-32. 

  9. Evatt ML. Oral glycopyrrolate for the treatment of chronic severe drooling caused by neurological disorders in children. Neuropsychiatr Dis Treat. 2011;7:543-7. 

  10. Wolff MS, Kleinberg I. The effect of ammonium glycopyrrolate (Robinul)-induced xerostomia on oral mucosal wetness and flow of gingival crevicular fluid in humans. Arch Oral Biol. 1999;44(2):97-102. 

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