Xylometazoline chemical structure
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Xylometazoline

Xylometazoline (Neo-Rinoleina®; Novorin®; Olynth®; Otriven®; Otrivin®; Xymelin®) is a topical decongestant that is directly dosed into the nose, either as a spray or as drops. more...

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Xylometazoline is marketed under the brand names Otrivine or Otrivin, with the standard adult dose being 0,1% w/v xylometazoline. The dose for children under 12 is 0.05%.

The drug works by constricting the blood vessels in the nose. The vasoconstriction means that there is less pressure in the capillaries and less water can filter out. This means that less discharge is made. (If the colour of the nasal passage is observed, it is visibly paler after dosage.)

Adrenaline does the same thing; xylometazoline is designed to look like adrenaline, and it binds to the same cell receptors adrenaline does. For this reason, it should not be used for people with high blood pressure, or other heart problems. (It acts mainly on alpha-adrenergic receptors.)

Unfortunately the vessels become resistant to the drug after prolonged dosing. The number of receptors decrease, and when the administration of the drug is ceased, chronic congestion can occur. Moreover long-term overdosing can cause degenerative changes in nasal mucous membranes that pose another health problem.

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Cocaine use in nasal surgery by ENT surgeons in Australia
From Australian Journal of Oto-Laryngology, 4/1/02 by Irani, Danesh

Objectives: To analyse the practices of Australian Otolaryngologists with regard to cocaine use in nasal surgery.

Methods: 400 questionnaires regarding cocaine usage during nasal surgery were mailed to all Australian Otolaryngologists.

Results: There were 150 responses. Ninety-six respondents (64%) routinely used cocaine in their work. Many of these mixed it with adrenaline, (49%) and 73% used it for all types of nasal surgery including FESS, rhinoplasty, septoplasty and turbinate surgery. Nearly all used between 150mg and 300mg of cocaine but modified their administration with medically unsuitable patients. Seven percent of respondents reported a major complication. Most of these events (68%) were anecdotal rather than in the surgeon's own experience, and were a single event in many years of usage. Some continue to use other agents mainly due to medico-legal implications of potential toxicity, cost of cocaine, or of maintaining a drug register with cocaine.

Conclusions: Cocaine is currently the most commonly used agent for nasal mucosal preparation in Australia and has had remarkably few reported adverse effects.

Key words: cocaine, nasal surgery, adverse effects

Introduction

Cocaine is benzoylmethylecgonine- a local anaesthetic of the ester type.1 It has been used as both a local anaesthetic and vasoconstrictive agent for intranasal surgery for over 100 years.2

Its most important action is its ability to block the initiation or conduction of the nerve impulse following local application. However, it also blocks the re-uptake of catecholamines, especially noradrenaline, at adrenergic nerve endings. This re-uptake process is responsible for terminating the actions of both adrenergic impulses and circulating catecholamines, and cocaine thus also produces sensitization to catecholamines, vasoconstriction and mydriasis. Other local anaesthetics do not share this property.

Its most striking systemic side-effect is stimulation of the CNS, producing a feeling of well-being and euphoria initially, but then followed by depression. Small systemic doses also slow the heart as a result of central vagal stimulation, but large doses cause an increased heart rate, due to increased central sympathetic stimulation as well the peripheral effects of cocaine on the sympathetic nervous system, discussed above. Hypertension, ventricular fibrillation, and other arrhythmias may occur, and a large intravenous dose may cause immediate death from arrhythmias, myocardial infarction or cardiac failure caused by direct depression of the heart muscle.3

Some surgeons have looked to other medications to achieve nasal mucosal preparation through concern to avoid cocaine. Reasons for this include its community reputation as an illegal drug, safety issues and the presence of alternate medicines. Other topical medicines have been used to induce vasoconstriction, including adrenaline, oxymetazoline, xylometazoline and phenylephrine, combined with lignocaine for anaesthesia. Factors that influence drug preference by the surgeon include safety, cost and effectiveness.

The objective of this survey was to analyse the practices of Australian Otolaryngologists with regard to cocaine use in nasal surgery.

Methods

400 questionnaires regarding cocaine usage during nasal surgery were mailed to all ENT surgeons and trainees in Australia.

Results

There were 150 responses to the 400 questionnaires.

96 of the 150 respondents (64%) use cocaine in nasal surgery. There was variation by state, with 87% of respondents in SA (13 of 15), 69% of respondents in both WA (11 of 16) and Victoria (24 of 35), and 68% of respondents in QLD (21 of 31) regularly using cocaine in surgery. However only 50% in both NSW (24 of 48) and Tasmania (2 of 4) regularly used this agent in nasal surgery. The only respondent from the ACT used this agent. The percent of surgeons using cocaine in surgery by state is shown in Figure 1.

69% (66 of 96) administer a dose of 150-300mg with 27% (26 of 96) using less than 150mg, and 2% (2 of 96) using more than 300mg. Two respondents use cocaine paste and did not quantitate the dose they use.

67% (64 of 96) of surgeons have administered cocaine for more than 10 years, with 20% (19 of 96) using it for 6 to 10 years and 13% (12 of 96) using it for 1-5 years.

The preferred agent for mixing is adrenaline (49% or 47 of 96), followed by co-phenylcaine forte (lignocaine and phenylephrine- 16% or 15 of 96), saline (7%) and drixine (oxymetazoline) (5%). 23% (22 of 96) prefer to administer plain cocaine only.

Of the surgeons who currently use cocaine in ENT surgery, 91 of 96 are using it in FESS (95%), with 83% (80 of 96) using it in septal surgery, 82% (79 of 96) in turbinate surgery and 81% (78 of 96) in rhinoplasty.

80% (77 of 96) of surgeons will modify their use of cocaine, usually if there is a history of cardiac arrhythmia (70% or 54 of the 77 who modify), or if their anaesthetist refuses to use cocaine in certain patients (66% or 51 of 77). 65% (50 of 77) modified the use in cases with ischeamic heart disease, and 49% (38 of 77) in patients with high blood pressure, while 36% (28 of 77) do so in patients with a history of cerebro-vascular disease.

20 of the 96 respondents (21%) who are using cocaine reported one or more adverse reactions in their series. The majority of these were minor (13 of 20), usually vasovagal effects including hypotension and fainting, hypertension, and tachycardia. Nausea and vomiting and agitation were also mentioned as minor side effects.

Major side effects were reported by only 7 surgeons and included cases of VT, SVT and bigeminy, with one surgeon reporting a case of abrupt loss of consciousness followed by paraplegia lasting 3 days, and another reporting a toxic reaction lasting 6 hours. There were no reported deaths.

54 of the 150 respondents do not use cocaine (36%). 43 have switched to another agent having once used cocaine, with 11 having never used it in. Of the 43 who have changed their practice, only 14 (33%) have done so due to personal experience of complications or of perceived risk of complications, the most common examples again being cardiac arrhythmias and vasovagal effects. 2 of the 14 were concerned about anosmia as a complication of cocaine administration.

The other 29 of 43 who no longer use cocaine cited other reasons for switching to another agent, such as the difficulty or inconvenience of maintaining a drug register, the need to lock up cocaine, the cost of cocaine, the fear of burglary, and of medico-legal concerns. 11 of this group of 29 gave their reason for no longer using cocaine as satisfaction with other agents that are available, usually co-phenylcaine but also lignocaine with adrenaline.

Discussion

Cocaine is the most popular mucosal agent for nasal surgery in Australia, being used by almost two thirds of Australian Otolarynngologists.

Cocaine is used in all forms of nasal surgery, but especially in FESS surgery. Nasal bleeding during surgery carries an increased risk of complications and increases the difficulty of surgery. Consequently surgeons place a high value on an agent that provides the best possible surgical conditions. This reduced risk of surgical complications must be weighed against the risks of side effects of cocaine. The high popularity of cocaine and the few reported complications attest to the general safety of cocaine, especially in light of modem anaesthetic advances and improved monitoring techniques.

The incidence of witnessed side effects is relatively small given the large case series undertaken by the survey group over many years. The low incidence may reflect some factors cited in the questionnaire, such as reducing the dose in higher risk patients and careful liaison with the anaesthetist during administration.

Cocaine is a form of anesthetic usually administered by the surgeon. As such the surgeon takes on some responsibility in using it. This starts with advising the patient that anaesthetics are being used, and checking that the patient is medically safe to have such an agent. During the case the surgeon will need to be aware of vital signs and liaise with the anaesthetist.

The safe maximum dosage of cocaine is reported to be 200mg or 1.5-3mg/kg 4,5. This dose applies to spraying cocaine or painting it directly onto the mucosa, and causes a more rapid absorption than application by patch or pledget. Clinical studies have shown that only approximately one third of a cocaine solution placed on pledgets is absorbed via the nasal mucosa, providing an added margin of safety for the surgeon 6.

11 of 29 of the respondents who have stopped using cocaine did so due to satisfaction with other agents. Several recent studies compare the analgesic and vasoconstrictor properties of cocaine to other agents.

Tarver et a1, using laser Doppler flowmetry to measure blood flow and testing sensation threshold and pain perception with Semmes-Weinstein monofilaments, concluded that 2% lignocaine plus oxymetazoline 0.025% is as effective or better than cocaine 4% at decreasing blood flow and providing anaesthesia, and hence an effective alternative to cocaine for nasal procedures.

Kasemsuwan and Griffiths8, using anterior rhinomanometry to assess changes in nasal resistance from decongestion and nasendoscopy to subjectively evaluate discomfort, concluded that 4% lignocaine with adrenaline (1:1000) solution is as effective as 10% cocaine, for intranasal procedures.

Lennox et a19, measuring peak nasal inspiratory flow using a Youlten peak flow metre to measure decongestion, and nasendoscopy to assess discomfort, concluded that cocaine 10% and co-phenylcaine (5% lignocaine, 0.25% phenylephrine) provide similar local anaesthesia and vasoconstriction of the nasal mucosa.

From these studies it appears that other agents may provide comparable conditions to cocaine when used for intranasal surgery.

However, most surgeons continue to use cocaine despite the availability of other agents, and enjoy the excellent conditions it provides and its very low rate of adverse reactions.

The following guidelines are included to assist the surgeon who is using cocaine for nasal surgery.

Guidelines

1. Check risk factors: cardiovascular disease (coronary artery disease, hypertension, arrhythmias), cerebrovascular disease, and previous adverse reactions. It should not be used in patients with thyrotoxicosis, or during pregnancy or breast-feeding.

2. Consent: Advise the patient that they are having anaesthetic agents with potential side effects.

3. Liaise with the anaesthetist when using cocainereduce the dosage if required.

4. Ensure that the patient is properly monitored during cocaine usage by oximetry, ECG and blood pressure monitoring.

5. The dosage for direct mucosal application is 1.5 to 3mg per kg. Higher doses may be used on pledgets or gauze application.

Conclusions

Cocaine is the most popular mucosal agent for nasal surgery in Australia. There are few side effects reported in a large study group. As with any medicine it should be used with an awareness of the contraindications.

References

1. REYNOLDS J.E.F. ed. Martindale. The extra pharmacopoeia. 30th ed. London: Pharmaceutical Press, 1993.

2. BEAUMONT G.D. The effects of topical cocaine and adrenaline anaesthesia of the nose combined with general anaesthesia. J Oto-Laryng Soc Aust 1974; 3:691-696.

3.HARDMAN J.G., LIMBIRD L.E. eds. Goodman and Gilman's The Pharmacological Basis of Therapeutics. 9th ed. New York: McGraw-Hill Co., 1996.

4. HOPKINS D.A.B. Anaesthesia: Recovery and Intensive Care. London: English Universities Press, 1970.

5. LEE J.A., ATKINSON R.S. Synopsis of Anaesthesia. 7th ed. Bristol: Wright, 1973.

6. GREINWALD J.H., HOLTEL M.R. Absorption of topical cocaine in rhinologic procedures. Larygoscope 1996;106:12231225.

7. TARVER C.P., NOORILY A.D., SAKAI C.S. A comparison of cocaine vs. lidocaine with oxymetazoline for use in nasal procedures. Otolaryngol Head Neck Surg 1993; 109:653-659.

8. KASEMSUWAN L., GRIFFITHS M.V. Lignocaine with adrenaline: is it as effective as cocaine in rhinological practice? Clin Otolaryngol 1996; 21:127-129.

9. LENNOX P., HERN J., BIRCHALL M. Local anaesthesia in flexible nasendoscopy. A comparison between cocaine and cophenylcaine. J Laryng Otol 1996; 110:540-542.

DANESH IRANI and MARTYN MENDELSOHN

Sdney

New South Wales, Australia

Danesh Irani M.B.,B.S., F.R.A.C.S. Fellow, Australian Academy of Facial Plastic Surgery Sydney, New South Wales

Martyn Mendelsohn M.B.,B.S., F.R.A.C.S. Department of Otolaryngology Royal Prince Alfred Hospital Camperdown, MSW, 2050

Correspondence:

Dr. Danesh Irani

449 Station Street

Carlton North, VIC, 3054

Ph: 0408 553 780

Fax: (03) 9816-9375

Email: drirani@hotmail.com

Copyright Australian Society of Otolaryngology Head & Neck Surgery Ltd. Apr 2002
Provided by ProQuest Information and Learning Company. All rights Reserved

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