Free «Promethazine» Essay Sample

Promethazine belongs to the group of drugs named phenothiazines. It influences the actions of chemicals in the human brain and functions as an antihistamine blocking the effects of the natural chemical histamine in the human body. Promethazine is used as an anti-nausea and sedative drug, which often appears in combinations with other medications. It is also helpful for the treatment of allergy symptoms and motion sickness. However, in case of overdose or misuse, the drug may cause serious adverse effects and even lead to fatal consequences. Although the abuse potential of promethazine is not thoroughly examined, its combination with opioids demonstrates a significant abusive effect. For this reason, promethazine is reviewed for its history, epidemiology, pharmacology, manufacture, effects, and subsequent treatment.

The Introduction of Promethazine

At the early stages of development, promethazine was used exclusively for medical purposes. This drug was first introduced in 1946 as a derivative of phenothiazine (Shapiro et al., 2013). Shapiro et al. (2013) mention that it was recommended for treatment of allergic reactions, nausea, and vomiting, pre- and post-operative sedation, adjunctive analgesia, and motion sickness. In 1949, promethazine was first combined with opioids in a form of a “lytic cocktail”, which consisted of chlorpromazine, promethazine, and meperidine (Shapiro et al., 2013). In modern practice, the combination of promethazine with opioids is not used for pre- and post-operative sedation due to its side effects and lack of information in support of its clinical effectiveness. In 1951, promethazine hydrochloride received approval of The Food and Drug Administration (Karabin, 2014). Since then, the drug has become widely used for the clinical purposes.

The Epidemiology of Promethazine

According to epidemiology studies, the cases of promethazine abuse are present in different groups of people throughout the world. Around 2000, the press reported on the abuse of cough syrup that contained promethazine and codeine by young people primarily in Texas (Shapiro et al., 2013). The presence of promethazine in fatal opioid overdoses was noticed in Kentucky in 2000-2004 when the drug was identified by autopsy in 14.2 % of methadone toxicity victims (Shapiro et al., 2013). In addition, 8.7 % of overdose death caused by depressants in the Seattle-King County area involved promethazine (Shapiro et al., 2013). Subsequently, the researchers registered the cases of intravenous use of promethazine by heroin addicts in Vietnam with the purpose of increasing an insufficient heroin dose or in the event of heroine’s absence (Shapiro et al., 2013). In India and China, promethazine abuse tendency was noticed in patients undergoing buprenorphine cure for opioid dependence (Shapiro et al., 2013). Thus, the cases of excessive non-medical use of promethazine have been reported worldwide.

The Pharmacology of Promethazine

The complex pharmacology, which makes its toxicological mechanisms not completely clear, characterizes promethazine. The drug is easily absorbed in the gastrointestinal tract and has 93 % protein-binding capability (Kee, Hayes, & McCuistion, 2014). Kee et al. (2014) also mention that promethazine is metabolized by the liver and excreted in urine and feces. The pharmacodynamics features of the drug are represented by blocking H₁-receptor sites on effector cells and impeding histamine-mediated responses (Kee et al., 2014). Promethazine does not resist histamine at H2 receptors (Cantisani et al., 2013). According to Cantisani et al. (2013), antihistamines put up resistance to nearly all smooth muscles stimulating effects of histamine on the H1 receptors of the large blood vessels, uterus, bronchial muscle, and gastrointestinal tract. In case of oral and intramuscular use, promethazine acts within 20 minutes and produces effect lasting from 4 to 6 hours (Kee et al., 2014). According to Kee et al. (2014), the onset of action of intravenous promethazine is 3 to 5 minutes with the same duration of effect as for the oral administration. Thus, the scientific study of promethazine reveals its histamine-antagonizing properties and the length of its influence on the human organism.

Promethazine Manufacture and Trade

Due to the demands of the global market, a large number of companies manufactures promethazine in different forms. Today, the drug is available in the form of tablets, syrup, suppository, and injections. Promethazine dioxide (dioxopromethazine) is used as the hydrochloride in the eye and nasal drops (Wisher, 2011). It is sold under the brand names of Avomine, Phenergan, Daralix, Fenazil, etc. (Wisher, 2011). The manufacturers of promethazine are Sanofi-Aventis (Australia), Wyeth (the USA), Aspen Pharmacare (South Africa), and Sella A. Laboratorio Chimico Farmaceutica (Italy) (Wisher, 2011). The US pharmaceutical company Morton Grove Pharmaceuticals markets promethazine (Karabin, 2014). In addition to them, many other companies practice the production of the drug in combination with other compounds.

The Expected Effects of Promethazine Use

In medicine, promethazine is used for the variety of purposes. According to Cantisani et al. (2013), this drug is helpful for the reducing of allergic symptoms since it produces the noticeable sedative effect. The use of promethazine can also reduce the symptoms of pneumonia, asthma, and other lower respiratory tract infections (Cantisani et al., 2013). In some countries, this drug is marketed for the sedative purpose, namely as a nasal sleep introducing the drug to sedate children, an anesthetic premedication causing sedation and reducing anxiety, and a dose-controlled transdermal remedy reducing nausea and vomiting after operations (Cantisani et al., 2013). Cantisani et al. (2013) also mention that promethazine is taken before traveling to prevent motion sickness and is a compound of cough-relieving medicament. With the proper dosage, it can bring antiemetic and antipruritic relief to patients. Promethazine has a marked melanogenesis-suppressing capacity due to which it can be used as a compound of skin-beautifying cosmetic and a skin-aging prevention agent (Cantisani et al., 2013). In some countries, everyone can get a 2 % promethazine cream without prescription to treat the allergic skin conditions, burns, and insect bites (Cantisani et al., 2013). Thus, this drug can produce various effects in combination with other components.

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Precautions against the Promethazine Use

In case of promethazine use, one should strictly follow the doctor’s prescriptions and pay attention to the circumstances that do not allow the administration of the drug. First of all, the treatment by the drug is forbidden in children under two years of age due to the association between phenothiazine sedatives and sudden infant death syndrome (Wisher, 2011). People who are allergic to it and suffer from asthma, glaucoma, heart or liver disease, high blood pressure, and stomach ulcer should not use this medicine (“Promethazine”, n.d.). In addition, the drug is not prescribed to those who have a history of seizures, enlarged prostate, and a weak immune system (“Promethazine”, n.d.). The neglect of these contraindications may lead to serious complications and even fatal consequences.

The Side Effects of Promethazine Use

The variety of promethazine’s pharmacological qualities contributes to the side effects produced by this drug. The general adverse effects of promethazine include drowsiness, dizziness, dry mouth, stuffy nose, blurred vision, constipation, ringing in the ears, impotence, and weight gain (Karabin, 2014). In children younger than two years old, promethazine may cause severe breathing problems or even death (Cantisani et al., 2013). Also, young children taking this drug may suffer from hallucinations, dystonias, excitation, and sometimes seizures (Cantisani et al., 2013). Cantisani et al. state that (2013) probably the most frequently occurring side effect of promethazine is sedation that ranges from mild drowsiness to deep sleep. Moreover, the misuse of promethazine may result in respiratory depression, hypertension or hypotension, tachycardia, and extrasystoles (Cantisani et al., 2013). Among the more serious adverse effects of promethazine one can name uncontrolled shaking, problems with balance or walking, easily bruising or bleeding, flu and fever symptoms, skin rash, problems with urination, swollen glands, and stomach pain (Karabin, 2014). In case of noticing any of these symptoms, it is necessary to stop taking promethazine and to consult the doctor. Therefore, together with desirable effects, the use of this drug may provoke unpredicted negative consequences that need medical attention.

Promethazine Dosage

The dosage of promethazine depends on its form and the symptoms it has to treat. The drug is presented in the tablet, syrup, suppository, and injectable forms (Karabin, 2014). Each of these forms requires special prescriptions for its use. In case of having an allergy, one should take 25 mg of promethazine one to four times a day before meals and at bedtime (Wisher, 2011). For the short-term management of insomnia, a patient should take 20 to 50 mg of promethazine hydrochloride at night (Wisher, 2011). For cold symptoms treatment, as well as vomiting and nausea prevention, the drug should be taken every four to six hours (Karabin, 2014). According to Karabin (2014), people who suffer from motion sickness should take promethazine 30 to 60 minutes before traveling and repeat the dose after eight to 12 hours. The recommended daily amount of promethazine for children aged 2 to 5 years is 5 to 15 mg (Wisher, 2011). A child of 5 to 10 years old can take to 10 to 25 mg every day. However, the need to take promethazine should be consulted with the specialists.

Promethazine Overdose

Similar to the majority of medications, promethazine can be taken in an excessive dose. The consequences of an overdose are different due to many factors including the promethazine dosage and its combination with other medications or substances. Most cases of isolated promethazine overdose are associated with delirium without fatal consequences. The common symptoms of promethazine overdose include dizziness, breathing problems, low blood pressure, fainting, lightheadedness, fast heartbeat, loss of consciousness, nightmares, dilated pupils, and loss of coordination (Karabin, 2014). In addition, promethazine should not be used in combination with amiodarone, sotalol, pimozide, quinidine, and procainamide due to the risk of abnormal heartbeat (Karabin, 2014). In rare cases, the promethazine overdose may lead to the sudden death (Monson, 2013). In case of taking promethazine, one should consider the dosage recommendations and the potential risk factors.

Promethazine Overdose Treatment

The ways of promethazine overdose treatment may vary. If the overdose occurred recently, the patient should take activated charcoal for the absorption of the drug in the digestive tract (Monson, 2013). Promethazine overdose may provoke the additional symptoms that require the subsequent supportive cure. According to Monson (2013), this kind of treatment includes fluids through an intravenous line, careful observation of the vital signs, and the use of medications like diphenhydramine to treat some specific symptoms of the overdose. All the consequent complications and side effects, which may occur, require the specific treatment options for every case. However, the most important thing in promethazine overdose treatment is timing since the patient has to be examined immediately after the detection of its symptoms.

In conclusion, the introduction of promethazine in the 1940’s marked the onset of its use for the variety of medical purposes. Today, promethazine is used as a component of different forms of medication and is manufactured by many companies worldwide. The use of this drug has proven to be helpful for the treatment of various health problems. However, a wide range of potential negative consequences of its use accompanies its numerous positive effects. For instance, in combination with opioids promethazine may produce an abusive effect. Moreover, the use of the drug in excessive amounts may cause overdose the consequences of which usually require additional treatment. Thus, like any other medication, promethazine should be taken strictly according to the prescriptions to avoid the side effects it may produce.