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Okay let’s talk about one of the most significant problems although it’s considered benign but often a reason for treatment discontinuation which is saya aria now many of you understand the pharmacology of the salivary glands and know that there are a number of muscarinic receptor subtypes which are expressed there but what we understand is that more likely than
Not the problem related to clozapine has to do with its metabolite nor clozapine which is also called in this methyl clozapine this turns out to be a muscarinic m1 agonist and we believe this is responsible for the drooling so although the parent compound clozapine may be an antagonist at a number of muscarinic receptors the metabolite is an agonist this is why we
Have people who are both constipated and drool at the same time we’re getting the mix properties of both the parent compound and the metabolites the evidence that it’s the m1 effects come from trials of parens appiah which is an m1 selective anticholinergic agent available mostly in europe but there are case reports and case series of people who were administered
Parens apini and this seemed to block the sia aria induced by clozapine so what’s the general approach to this occasionally you can try dose reduction but often this does not get you much mileage we prefer in the state hospital system always starting with locally applied agents as we will discuss constipation is an enormous problem in patients with clozapine and
One does not wish to add to this anticholinergic burden through the unnecessary use of systemic anticholinergics unless it is absolutely necessary the starting treatments are either atropine 1% ophthalmic drops administered sublingually not in the eye sublingually the slides here say 1 to 2 drops initially at bedtime and up to tid and we will certainly go even to 3
Drops as needed up to tid if that’s what we need to get good control of the say our ria if that doesn’t work the other option is i petroleum spray again this was developed as a nasal spray but you’re gonna spray it in the mouth and use the higher strength which is point zero six percent again you can go up to three sprays tid and the reason to manage this is that
There is a literature out there about patients on clozapine having increased risk for pneumonia and we think this has to do with aspiration events which may occur at night and of course for people who drool there’s also the social problem of their appearance in public so it’s really something to be attentive to and be very aggressive at treating if the locally
Applied agents simply do not work then one has ample justification for going to the systemic drugs knowing that you are incurring a burden of increased risk of constipation so one option includes like a pyro weight we prefer this over other agents such as bench chopping simply because glyco pyruvate does not cross the blood-brain barrier so you are not going to
Incur the central anticholinergic effects which one might get from been strobing or arcane or other anticholinergic anti parkinsonian medications the usual dose is two to four milligrams at night one can go up to slightly higher doses it is worth knowing though that there is an alternative to glycol pyruvate which can be considered in certain patients if their
Blood pressure will tolerate it and this is the use of the alpha-1 antagonist or as ascend the doses which have been studied are relatively modest one milligram at bedtime would be the starting dose if this is tolerated one can after one to two weeks go up to two milligrams the biggest risk of course is going to be ortho stasis but the advantage is that if this
Works you avoid all of the peripheral anticholinergic effects of a medication such as like a pyro leg if somebody has a partial response to the locally applied agents these should be kept on board while you’re adding the other agent whether it’s to razz us in or then later on like a pyro late but it is important to get on top of this again this may be a reason that
The patient will say i don’t want to take this medicine a and b it may present a risk for aspiration pneumonia later on so to summarize salary apresentava aurélie applied medication such as attribute 1% drops where i petroleum point zero six percent spray are preferred as they do not increase constipation risk for the same reason consider trying low dose to reduce
In before using like a pyro wait if the orally applied medications are not sufficiently effective
Transcribed from video
Clozapine-Induced Sialorrhea: Why Is It Important and How Should You Manage It? By Psychopharmacology Institute
