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Topical Diltiazem in Management of Chronic Anal Fissure: a Review of the Literature

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Topical Diltiazem in Management of Chronic Anal Fissure: a Review of the Literature Clinical Trial Outcomes 4 Clinical Trial Outcomes Topical diltiazem in management of chronic anal fissure: a review of the literature Clin. Investig. (Lond.) Anal fissure is a common painful anorectal condition which affects people of various Roja Hadianamrei age groups, and deteriorates their quality of life. Chronic anal fissure requires medical Department of chemistry, intervention either by pharmacotherapy or by surgery. Various pharmacological agents Loughborough University, Loughborough, Leicestershire, UK have been used in the treatment of chronic anal fissure with the aim of relaxation of Tel.: +44 (0)782 641 1626 internal anal-sphincter smooth muscle. Diltiazem is a calcium-channel blocker that [email protected] has been tried in several clinical studies for management of chronic anal fissure. This review focuses on the available literature data on the use of topical diltiazem (cream, gel, ointment) in the treatment of chronic anal fissure in order to give an overall viewpoint of the work carried on in this field and the results obtained. Keywords: anal fissure • cream • diltiazem • gel • ointment • topical Anal fissure hand, persist for more than 6–8 weeks and Definition, symptoms have different morphological manifestations Anal fissure represents one of the most com- including ulcer with keratinous edges, presence mon anorectal problems encountered in of a sentinel tag at the external apex, hypertro- practice. An anal fissure is a linear, longi- phied anal papillae and exposed internal anal- tudinal tear or split in the epithelial lining sphincter smooth-muscle fibers [1,3–6]. CAF of the distal anal canal [1–3] . The commonly often require medical intervention including accepted definition of anal fissure is: ‘A lin- surgery or pharmacotherapy. ear ulcer of the anoderm, distal to the den- tate line, generally located in the posterior Etiology midline’ [4]. During defecation, the lesion The etiology of anal fissure is not so clear. Pre- is stretched causing severe sharp pain, often viously, anal fissure was thought to be due to 10 described as ‘passing broken glass’ and a severe constipation or straining at defecation. burning pain which can persist for several However, current evidence shows that anal hours after defecation and be accompanied fissures are associated with increased tone by bleeding [3–5]; pruritus, swelling, prolapse and spasm of the internal anal sphincter [5–7]. 2014 and discharge is also present in a minority of Thus, it is suggested that the primary cause patients [6]. of CAF is increased resting anal pressure, causing a reduction in anodermal blood flow Classification by compressing the blood vessels which pass Fissures can be classified as acute or chronic, through the sphincter, which eventually leads based on both chronology and morphology. to ischemic ulceration of anal mucosa [2,3,6]. Anal fissures are considered to be acute if they have been present for less than 6 weeks, super- Medical therapy ficial and have well-demarcated edges. Most The goal of medical treatment for CAF is to of the acute anal fissures heal spontaneously achieve a temporary reduction of pressure of or with conservative medical management. the anal canal to facilitate the healing of the Chronic anal fissures (CAF), on the other fissure (reversible sphincterotomy), thereby part of 10.4155/CLI.14.86 © 2014 Future Science Ltd Clin. Investig. (Lond.) (2014) 4(10), 923–934 ISSN 2041-6792 923 Clinical Trial Outcomes Hadianamrei reducing muscle tone [4]. This can be achieved by surgi- Pharmacokinetics cal techniques such as anal dilatation, posterior mid- Diltiazem is absorbed almost entirely from the gas- line sphincterotomy, lateral internal sphincterotomy or trointestinal tract after oral administration. However, by pharmacotherapy. Surgical techniques are generally due to extensive first-pass hepatic metabolism, pri- associated with risk of permanent fecal incontinence. marily by the cytochrome P450 isoenzyme CYP3A4, Therefore, since the early 1990s, nonsurgical methods only about 40% of an oral dose is bioavailable. This for treatment of CAF emerged, generally referred to as also causes considerable interindividual variation in ‘chemical sphincterotomy’. Chemical sphincterotomy is plasma concentrations. Generally peak plasma con- mainly based on reducing internal anal-sphincter spasm centrations are achieved 3–4 h after oral intake. The (resting anal pressure) and/or increasing improving vas- plasma protein binding of DTZ is approximately cularity of internal anal muscle by various mechanisms 80%. It is distributed into breast milk which limits using pharmacological agents. its use during lactation. The elimination half-life of The greatest advantage of chemical sphincterotomy DTZ is reported to be 3–5 h. It is mainly excreted over surgical techniques is avoiding the risk of perma- as metabolites in bile and urine with a small por- nent impairment of continence [3,5]. Various pharma- tion (2–4%) being excreted as unchanged drug in cological agents have been used for chemical sphincter- urine [8]. However, no information about the pharma- otomy including glyceryl trinitrate (GTN), isosorbide cokinetic parameters of topical DTZ could be found dinitrate, botulinum toxin, calcium-channel block- in the literature. A registered clinical trial aimed at ers (CCB) such as nifedipine and diltiazem (DTZ), assessing the single- and multi-dose pharmacokinet- lidocaine and bethanecol [6]. ics of oral DTZ and topical DTZ is ongoing, but not Contraction of the internal anal-sphincter smooth- completed yet [9]. muscle depends on increased intracellular calcium concentration, which is mediated either by calcium Drug interactions influx through calcium channels or by stimulation of Concomitant administration of DTZ with amioda- α1-adrenoceptors. Thus, relaxation of these muscular rone, β-blockers, digoxin and mefloquine may result cells can be achieved by directly decreasing intracellu- in increased depression of cardiac conduction and risk lar calcium concentration through blockade of calcium of bradycardia or atroventricular block. Enhanced channels, as well as increasing cGMP and cAMP [5]. antihypertensive effect may occur with concomitant Therefore, CCB such as nifedipine and DTZ are sup- use of other antihypertensive drugs and antipsychot- posed to be effective in treatment of CAF by decreasing ics. DTZ may interact with drugs sharing the same the influx of calcium into the internal anal-sphincter metabolic pathway, with enzyme inducers such as smooth-muscle cell, leading to muscle relaxation and carbamazepine, phenobarbital, phenytoin and rifam- reduction in resting anal pressure. picin, and with enzyme inhibitors such as cimetidine and HIV-protease inhibitors [8]. Diltiazem Diltiazem is a benzothiazepine CCB. It is a peripheral Precautions and coronary vasodilator with limited negative inotropic Diltiazem is contra-indicated in patients with the sick activity and inhibits cardiac conduction, particularly at sinus syndrome, pre-existing second or third degree the sino-atrial and atrioventricular nodes. DTZ is given atroventricular block, or marked bradycardia, and orally for the management of angina pectoris and hyper- should be used with caution in patients with lesser tension once, twice or three-times daily. It is also admin- degrees of atroventricular block or bradycardia. DTZ istered by intravenous route in the treatment of various has been associated with the development of heart cardiac arrhythmias such as atrial fibrillation, atrial failure and great care is required in patients with flutter and paroxysmal supraventricular tachycardia [8]. impaired left ventricular function. Treatment with DTZ should commence with reduced doses in elderly Mechanism of action patients and in patients with hepatic or renal impair- CCB cause smooth-muscle relaxation by blocking slow ment. Due to teratogenic effects observed in animals, L-type calcium channels, thus preventing the influx its use should be avoided during pregnancy [8]. of calcium into the smooth-muscle cell, and decreas- ing intracellular calcium concentration [3,5,8]. This Methods reduces the amount of calcium available to combine The aim of this review was to summarize and com- with calmodulin and subsequently prevents activation pare the currently available literature data on the of the myosin light-chain kinase required for smooth use of topical DTZ (ointment, gel, cream), for the muscle cell contraction [5]. treatment of anal fissure, in order to determine the 924 Clin. Investig. (Lond.) (2014) 4(10) future science group Topical diltiazem in management of chronic anal fissure Clinical Trial Outcomes effectiveness of DTZ as an agent for chemical sphinc- excluded if no translations were available. The retro- terotomy, either individually or in comparison with spective studies, studies with same study population other therapeutic agents or surgical treatments. and similar systematic reviews or meta-analyses were All prospective clinical studies including ran- excluded. domized clinical trials (RCTs), pilot studies and The keywords used for search were DTZ, topi- nonrandomized interventional studies that evalu- cal, cream, gel, ointment, anal fissure and different ated the effectiveness of topical DTZ (in the form combinations of them. The following databases were of cream, gel or ointment) in the treatment of anal searched for published data using different combina- fissure, either individually or in comparison with tions of the above-mentioned keywords: Medline, other
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