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Файл:Ординатура / Хирургия / Библиотека им академика М.И. Перельмана / Книга_5536_Библиотеки_им_академика_М_И_Перельмана.pdf
Overview of Drugs
■ Administration: Disulfiram is initially dosed at 500 mg/day for one to two
weeks, followed by an average maintenance dose of 250 mg/day with a
range from 125 to 500 mg based on the severity of adverse effects. The
medication should not be used by patients with current alcohol intoxication.
Patient education should address “hidden” forms of ethanol (eg, tonics
and mouthwashes) and the duration of the drug’s activity (up to 14 days
after stopping).
■ Efficacy: A 2014 meta-analysis of two clinical trials with a total of 492
patients did not find a significant difference between disulfiram and placebo
in return to any drinking or other primary substance use disorder (SUD)
outcomes. A systematic review found mixed results in one large trial and
three smaller trials of disulfiram versus placebo for alcohol dependence. The
large study, a 52-week, multi-site trial of 605 US veterans, found disulfiram
to be no more effective than placebo in maintaining abstinence or in time
to first drink, but it may have reduced drinking days in a subgroup that
drank during the study. A high rate of noncompliance with medication
was seen. A subsequent study suggested that disulfiram is effective when
the medication is taken routinely under supervised conditions. In a trial,
243 patients with alcohol dependence were randomly assigned to receive
disulfiram, naltrexone, or acamprosate with regular supervision over a 12week period. Compared with patients taking naltrexone or acamprosate,
patients taking disulfiram experienced a greater reduction in heavy drinking
days and average weekly consumption, and a longer time to first drink.
The relative benefits of disulfiram were less prominent in a subsequent,
unsupervised treatment period of up to 52 weeks.
■ Adverse effects: Side effects of disulfiram are usually minor, including
fatigue, mild drowsiness, headache, and dermatitis. Severe adverse reactions
are rare, but include psychosis and hepatitis. Patients receiving disulfiram
should be monitored for hepatotoxicity.
Disulfiram, an aldehyde dehydrogenase inhibitor, has been approved by US FDA in
1951 as an aversive therapy for the management of alcohol dependence. It blocks
the oxidation of ingested alcohol at the acetaldehyde stage and prevents its rapid
metabolism to acetate. Thus when a disulfiram treated patient ingests even small
amounts of alcohol, acetaldehyde accumulates as a result of the disulfiram-ethanol
reaction and causes tachycardia, hypotension, diaphoresis, flushing, dyspnea, nausea
and vomiting. These symptoms act as a deterrent to alcohol ingestion. Disulfiram
is available as 250mg tablets with the recommended dosage being 250-500mg per
day. Disulfiram is often not recommended as the first line medication for newly
diagnosed alcohol dependent patients but is reserved for treating patients who have
previously failed one or more courses of treatment or those who are motivated to
achieve complete abstinence. With the advent and emergence of Naltrexone and
Acamprosate, there has been a decline in Disulfiram use with it slipping to a second
line treatment in many centers for the treatment of alcohol dependence. Safety
concerns may also be the reason for this as many alcoholic patients try to consume
alcohol even when on Disulfiram and hence may cause themselves unnecessary
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harm. Disulfiram is a prescription medication that generates a heightened sensitivity
to alcohol; it is used to help those with severe alcohol problems curb their drinking.
Sold under the brand name Antabuse®, disulfiram is considered an antialcoholic
drug due to its production of a strong reaction to the presence of alcohol in the
system. Commonly prescribed as an alcoholism medication, emerging research
suggests it may also be beneficial in treating chronic cocaine addiction.
Illustrated Handbook of Drugs & Alcohol Related Health Issues
Ciattion: http://images.wisegeek.com/alcoholic-drinks-on-bar-counter.jpg
This medication works by inhibiting production of the enzyme in the liver that breaks
down alcohol; it also averts the proper breakdown of the neurotransmitter dopamine.
If alcohol is consumed and comes into contact with disulfiram, a severe reaction
typically occurs. The reaction is caused by the concentration of the inhibited liver
enzymes in the blood, and the effect is often one of an acute, virtually instantaneous
hangover. It can last anywhere from a half hour to several hours.
The body responds in several ways to the convergence of disulfiram and alcohol
in the system. The first sign is usually flushed skin and a rapid heart beat. These
symptoms can quickly escalate to dizziness, vomiting, visual and auditory problems,
headache, disorientation, and, in extreme cases, failure of the circulatory system.
Disulfiram was invented in 1948 by scientists at a Danish drug company. Its discovery
was purely unintentional; the researchers had been hoping to find a treatment for
parasitical infections. The drug’s antialcoholic effects were soon evident, and it was
marketed around the world as an aid to drinking cessation.
Patients taking disulfiram are advised not to take the drug if they consumed alcohol
in the preceding 12 hours. The medication builds up in the system, and the body
develops no tolerance to it; in fact, over time, its effects only strengthen. Patients
Overview of Drugs
who stop taking disulfiram have found that the drug can stay in the system for up
to 14 days after the last dosage.
Disulfiram is administered in small round tablets bearing the letter “A.” They are
available in 200 mg, 250 mg, and 500 mg pills. The majority of patients are
prescribed 500 mg in a single daily dose for a period of two weeks. After the two
week period, a doctor will typically adjust the dosage as necessary to establish a
healthy daily amount for regular intake. While on disulfiram, doctors encourage
patients to utilize other modes of alcoholic treatment to support long-term sobriety,
including therapy, support groups, and lifestyle changes.
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Pharmacotherapies for Opioid Dependence
The development of effective treatments for opioid dependence is of great importance
given the devastating consequences of the disease. Opioids, used medically for
pain relief, have analgesic and central nervous system depressant effects, as well
as the potential to cause euphoria. Opioid use disorder can involve prescribed or
nonprescribed use of pharmaceutical opioids or use of illicitly obtained heroin. Opioid
use disorder is typically a chronic, relapsing illness, associated with significantly
increased rates of morbidity and mortality.
In patients with opioid use disorder who have achieved abstinence through medically
supervised withdrawal or other means, there are medication and nonmedication
options for long-term maintenance treatment. Medication treatment is often much
more effective in opioid use disorder compared with abstinence-based therapy, a
nonmedication treatment.
Citation: https://www.ncadd.org/images/easyblog_articles/2024/109725978.jpg
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Maintenance pharmacotherapy for opioid use disorder is reviewed here. The
epidemiology, pharmacology, clinical manifestations, course, screening, assessment,
diagnosis, and psychosocial treatment for opioid use disorder are discussed separately,
as are topics on medically supervised opioid withdrawal, prescription drug misuse,
substance use disorder in physicians, and treatment of acute pain in the patient
chronically using opioids:
Illustrated Handbook of Drugs & Alcohol Related Health Issues
Buprenorphine
Buprenorphine is a prescription narcotic that is used as a treatment for heroin
addiction. Although it might seem counterintuitive to treat addiction to an opiate with
another opiate, this treatment can effectively reduce both physical and psychological
dependency on heroin. In addition, this medication also is prescribed to treat severe
acute or chronic pain.
This medication is an effective treatment for heroin addition for two reasons. First,
it is able to prevent withdrawal symptoms caused when someone who is physically
dependent on heroin stops taking the drug. The second reason is that buprenorphine
blocks the narcotic effects of heroin, preventing the user from experiencing the high
that heroin normally would provide.
Buprenorphine works in this way because it is a partial agonist of other opioids. This
means that it competes with other opioids for the cellular receptors that enable cells to
respond to opiate drugs. When this medication is taken, it therefore reduces the effects
of any other opioid drugs that also are used. As a result, the heroin user’s reason for
using heroin is mitigated. This type of heroin withdrawal treatment is effective because it
allows the heroin user to make changes in his or her life without suffering the debilitating
cravings and physical symptoms of heroin withdrawal.
Ciattion: http://images.wisegeek.com/cooked-heroin-in-spoon-with-syringe.jpg
Overview of Drugs
One particular advantage of this medication is that even at low doses, it is a potent
enough partial agonist that it can compete strongly with heroin for available receptor
sites. This means that even a low dose of the medication can eliminate cravings
in someone who is addicted to heroin. Another advantage is that this medication
has a so-called “ceiling effect,” which means that the effects of the drug increase
with higher doses but plateau relatively quickly. As a result, buprenorphine is less
addictive and has fewer side effects in comparison to many other opiates.
Even so, this medication can be addictive and subject to abuse in people who do not
have a physical opioid addiction. In addition, this medication can cause a range of
side effects. Most of these are common to all opioids, including constipation, nausea
and vomiting. Initial treatment with this medication also can cause a withdrawal
syndrome, symptoms of which include nausea, vomiting, muscle cramps, diarrhea,
insomnia, sweating, irritability, distress and opioid cravings.
Buprenorphine is a much more effective treatment for heroin dependency when it is
used in conjunction with a comprehensive support plan. This is important because
there normally are multiple factors contributing to heroin use and dependency.
Therefore, a treatment plan typically includes counseling and development of a
support network, in addition to medication.
A strong opioid analgesic with both partial agonist and partial antagonist properties.
It is an alternative to methadone for withdrawal and maintenance treatment, and
has a much lower risk of death from overdose than methadone. Buprenorphine is
listed on the PBS as S100 under Section 100 of the National Health Act 1953 and
is approved by the Therapeutic Goods Administration (TGA).
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Buprenorphine Hydrochloride
Buprenorphine hydrochloride is classified as an opioid, which means that it is in
the same chemical family of morphine, codeine, and heroin; however, it has the
distinction of producing less euphoric effects than these drugs. It is available as
a tablet, which is used to treat opioid dependence, and as an injection, which is
used as an analgesic for treating moderate to severe pain. As it is a medication
capable of causing serious side effects and even death, it should only be taken
under a doctor’s supervision. Those who take this drug should be aware of special
instructions to follow and what the correct dosage should be, as well as the
medication’s extensive list of side effects and precautions.
The recommended dosage of buprenorphine hydrochloride should be strictly adhered
to by the patient. Adults may receive a tablet dosage of 12 to 16 mg per day,
while adults and children over the age of 13 may receive 0.3 mg in an injection
every six hours, as needed. Overdosage is extremely dangerous, since it can cause
respiratory depression, low blood pressure, and death.
Patients and their families or caregivers should know the correct method of taking
buprenorphine hydrochloride and also be familiar with the measures that they
must take to reduce the likelihood of dangerous effects. Instead of swallowing
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the tablets, which hinders effectiveness, the tablets should be placed under the
tongue until the medication dissolves. Also, the dosage should not be altered and
patients should never stop taking the drug unless they have been told to do so by
their doctor. Abstaining from alcohol and other central nervous system depressants,
such as sleeping pills or narcotics, will help to avoid a life-threatening overdose.
Additionally, patients should either avoid or exercise great care in driving or engaging
in activities that require mental alertness.
Illustrated Handbook of Drugs & Alcohol Related Health Issues
Citation: http://www.clinixplus.net/product_images/r/749/burepen_1__72844.jpg
Due to the serious nature of buprenorphine hydrochloride, patients should be alert
to the manifestation of side effects it can cause. Cardiovascular effects include
high or low blood pressure, along with a fast or slow heartbeat. Central nervous
system effects involve dizziness, sedation. and confusion, as well as hallucinations,
psychosis, and coma. Gastrointestinal side effects of buprenorphine hydrochloride
include nausea, vomiting, and constipation, along with loss of appetite, diarrhea.
and abdominal pain. Other symptoms include slow or shallow breathing, constricted
pupils, and hepatitis, in addition to rash, itching, and infection.
In addition to the side effects, certain precautions should be considered when
taking buprenorphine hydrochloride. As it has abuse potential, psychological and
physical dependence can develop, along with tolerance. Elderly and debilitated
patients are more susceptible to the adverse effects, so the drug should be used
cautiously in these groups. It also should be used carefully in those with various
medical conditions, some of which include impaired liver, kidney, or lung function,
as well as central nervous system depression, coma, or toxic psychosis. Another
group that should use the drug only with caution is head injury patients, as it can
increase pressure within the head.
Methadone
This is a long-acting synthetic opioid which can be used for both withdrawal and
maintenance treatment. It decreases the need for heroin-dependent individuals to
Overview of Drugs
regularly use intravenous opioids. Methadone maintenance programs monitor drug
use and should provide ongoing counselling and support. Methadone is listed on the
PBS as S100 under Section 100 of the National Health Act 1953 and is approved
by the Therapeutic Goods Administration (TGA).
Methadone is a prescription drug used most commonly to relieve pain and treat
withdrawal symptoms from opioid drugs such as heroin. It is similar to morphine,
but is less addictive to the patient. This drug has been widely studied, and it is
used in many drug addiction recovery programs.
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Citation: http://images.wisegeek.com/syringe-with-cooked-heroin-and-spoon.jpg
The reason that methadone works is that it replaces the need for an opiate in the
brain. When an individual is addicted to heroin or a similar narcotic, an excess
of dopamine is released into the body. Addiction is caused by the user’s need for
continuous occupation of the opioid receptor by an opiate. Methadone occupies this
receptor and stabilizes dopamine production, allowing the user to safely detoxify
from heroin or other opioids while keeping withdrawal symptoms at bay.
Ultimately, the patient will become dependent on this drug instead of heroin. This
is regarded by the medical community as beneficial, however, as the individual is
free of the compulsive and detrimental behavior of a heroin addict. Many addicts
will require a long-term continuous treatment plan, often taking several years, to be
free of any type of opiate addiction. Methadone is simply the first step on that path.
According to the American Office of National Drug Control Policy, methadone is
a safe and effective medication for treating narcotic dependence. It must be used
under the supervision of a medical professional, as abuse can result in serious side
effects. If used properly, this treatment will not interfere with cognitive functions,
mental facilities, or ordinary day-to-day activities. It is not a sedative or intoxicant,
but instead relieves the cravings experienced by opiate addicts without causing a
“high.”
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Illustrated Handbook of Drugs & Alcohol Related Health Issues
Citation: http://images.wisegeek.com/pills-and-beer.jpg
Minor side effects of this drug include constipation, excessive sweating, drowsiness,
and water retention. Once a tolerance is established, these symptoms typically
subside. If the drug is abused, however, it can cause slowed breathing that can
result in death. It should also not be combined with alcohol, as this can cause
dangerous side effects or death. The dosage instructions provided by a healthcare
professional should never be exceeded, and individuals should never stop taking
the drug suddenly.
Some individuals may not be able to safely take methadone, including women who
are pregnant or nursing. It can cause harm to an unborn baby, including addiction
or withdrawal symptoms after birth, and can be passed through the breast milk from
mother to child. People with asthma, COPD, or other breathing disorders should not
take this drug, nor should sufferers of liver or kidney disease, bowel obstruction,
epilepsy or other seizure disorders, low blood pressure, or gallbladder disease.
Levoalphaacetylmethadol (LAAM)
LAAM is a synthetic opioid analgesic which acts similarly to methadone. It is longacting and only needs to be taken three times per week. Overseas trials suggest
that LAAM is as safe as methadone and has similar treatment outcomes and patient
retention. This drug is not available for use in Australia.
Overview of Drugs
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Naltrexone
This is a competitive opioid antagonist, which completely blocks the effects of opioids
for 24 to 72 hours. Maintenance therapy is suitable for highly motivated patients
who wish to remain abstinent, are socially and psychologically stable and have
good social support. Naltrexone is not listed on the PBS for opioid dependence but
is approved by the TGA as an adjunctive therapy. Clinical trials are also underway
using naltrexone for rapid detoxification.
Withdrawal and Detoxification
Detoxification is withdrawal from a drug in a supervised way in order to minimise
withdrawal symptoms and risks related to withdrawal. Details of withdrawal
management are covered in the management and intervention sections of relevant
chapters on specific drugs.
Effective withdrawal management may be performed in the home supported by the
GP, other health workers and non-using supportive relatives or friends.
This form of withdrawal management depends on:
■ the drug of dependence
■ the severity of the dependency
■ the wishes of the patient
Home-based withdrawal management should be considered:
■ when there is no evidence of severe withdrawal, e.g. tremor, hallucinations,
disorientation
■ where there is no past history of delirium tremens or of fits
■ in the presence of supportive relatives who elect to stay with the patient
during the period of detoxification
■ when there is no evidence of a medical illness such as pneumonia or
pancreatitis
■ when no previous history or evidence of suicide is contemplated
■ where the patient does not have access to the drug from which they are
being withdrawn
Withdrawal can be medicated (assisted by the use of controlled sedatives) or nonmedicated. The latter is appropriate for patients who have no co-existing medical
disorders and when only a mild withdrawal can be anticipated.
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Ciattion: https://beachway-leadtoconversion.netdna-ssl.com/wp-content/uploads/2016/06/
Illustrated Handbook of Drugs & Alcohol Related Health Issues
alcohol-withdrawl-symptoms.jpg
In cases of multiple drug use, patients may not wish to withdraw from all substances
at the same time. Withdrawal management should be part of an ongoing treatment
program linked to coping and relapse prevention strategies.
Intoxication and Overdose
Intoxication is defined as the intake of a quantity of a substance which exceeds the
individual’s tolerance. Overdose is defined as the state that occurs when a person
has ingested a quantity of a drug that exceeds tolerance and produces behavioural
and physical abnormalities.
When presented with an intoxicated or overdose patient the priority is ABC First
Aid procedures:
■ A — Airway
■ B — Breathing
■ C — Circulation/cardiac
In acute overdose it is recommended that patients are closely observed, monitored
and referred to an acute hospital. Do not assume that alcohol or drugs are the sole
cause of the patient’s coma.
Other possible causes include:
■ trauma
■ epilepsy
■ metabolic abnormalities – diabetes, hepatic failure, hypercalcaemia, renal