Treatment of Alcoholism

inhibits acetaldehyde dehydrogenase. Minimal amounts of alcohol will cause “disulfiram reaction” – severe HA and sweating and flushing and hypothermia!.This is a NASTY drug! This is used to deter the patient from using alcohol!!

Treatment of Alcoholism

lowers activity of receptors for glutamate-maintenance of abstinence.

Treatment of Alcoholism

for alcohol withdrawal to prevent delirium or seizures – delirium tremens can occur in alcohol withdrawal patients! You MUST ensure that the patient is NOT taking any other alcohol when taking Benzodiazepines

Treatment of Alcoholism

for alcohol withdrawal to reduce tremors and reduction of heart rate and blood pressure

Major characteristics

Powerful addictive stimulant*

Source- leaves of the Erythroxylon coca, schedule II -high potential for abuse

Physical forms – hydrochloride salt and free base (2 forms)

Hydrochloride salt or powdered form of cocaine, dissolves in water can be taken IV or intranasally

                               “coke”, “snow”, “flake”

CRACK-is the street name given to the free base form of cocaine that has been processed from the hydrochloride form to a smokable substance – this is usually buffered in some sodium bicarb!!

If you INHALE cocaine HYPOCHLORIDE you get certain peak plasma levels. If you INHALE FREE BASE cocaine it gets MUCH MORE peak plasma levels!!

MOA

Blocks dopamine transporter.

Blocks both NE and serotonin re-uptake

RAPID absorption*

Rapid metabolism and elimination.

                            ↓

                benzoylecgonine

Benzoylecgonine can remain in urine for 5-8 days after the drug is stopped! Hence, this metabolite is key!!

SHORT-term effects

Increased energy

Decreased appetite

Mental alertness – this is produced by the DA and 5-HT that is around!!

Increased heart rate and blood pressure

Constriction of blood vessels

Increased temperature

Dilated pupils – very dilated!!

LONG-term effects

Addiction

Irritability and mood disturbances

Restlessness

Paranoia

Auditory hallucinations

Other effects

Loss of smell sensation, nosebleeds, problems with swallowing, hoarseness, irritation of the nasal septum, chronically inflammed runny nose

Ingested cocaine – severe bowel gangrene – this is a problem with transporters

IV users – allergic RXNs (apart from injection site reactions like HIV. Notice how in 5% of patients, you will see Steven Johnson’s Syndrome!!)

Lack of appetite, weight loss and malnourishment

Symptoms of Withdrawal

Dysphoria, depression

Sleepiness, fatigue

Cocaine craving

Bradycardia

Gradual diminution of these over 1-3 weeks

Maternal and fetal complications

Maternal complications include malignant hypertension, cardiac ischemia, cerebral infarction, and sudden death.

Fetal effects include spontaneous abortion and death in utero.

High risk of premature rupture of membranes, preterm labor and delivery, IUGR, abruptio placentae.

Newborns display tremens, irritability and suckling problems.

Cognitive and neurobehavioral problems

Lack of coordination

Visual problems.

Marijuana

General Characteristics

pot”, “grass”, “weed”

Greenish-gray mixture of the dried, shredded leaves, stems, seeds and flower of Cannabis sativa (users smoke in hand-rolled cigarettes called joints)

“Combos”------- plus coke.

                ------- plus bevs.

ACUTE effects

Rapid heart beat, bronchial passage relaxes and become enlarged, blood vessels in the eyes dilate.

Increased pulse rate, and reddening of the conjunctiva***

Euphoric or “high” by acting in the brain’s reward system

Impairs ability to form memories (Anterograde Amnesia), recall events, and shift attention from one thing to another

Disrupt coordination and balance – this happens when you take higher doses

HIGH doses may experience acute toxic psychosis (hallucination, delusions and depersonalization – a loss of the sense of personal identity or self-recognition)

Other effects

Burning, stinging of the mouth and throat, often accompanied by a cough

Cough and phlegm production, more frequent acute chest illnesses, heightened lung infections, greater tendency toward obstructed airways*

LSD (Lysergic acid diethylamide)

Mescaline

Psilocybin

General Characteristics

Profound distortions in a person’s perceptions of reality

Under the influences of hallucinogens, people see images, hear sounds, and feel sensations that seem real but do not exist

Some compounds in this category produce, rapid emotional swings

MOA

Stimulation of presynaptic and postsynaptic serotonin receptors.

General Characteristics

MOST POTENT hallucinogenic drug***

Clear, white, odorless water-soluble synthesized material chemically related to the ergot alkaloids

Sold on the illicit market in a variety of forms-a popular system is postage stamp-sized papers impregnated with varying doses of LSD

Pharmacokinetics

Rapidly absorbed* with effects beginning at 40-60 minutes (25 µg), peaking at 2-4 hours, gradually returning to baseline over 6-8 hours

Clinical Symptoms

At doses of 100mg, LSD produces perceptual distortions and sometimes hallucinations; mood changes (elation, paranoia and depression), intense arousal, and sometimes a feeling of panic*

Pupillary dilation, increased blood pressure and pulse, flushing, salivation, lacrimation and hyperreflexia

VISUAL effects* are prominent; color seems more intense and shapes may appear altered – they will see halos and such!

Phencyclidine (PCP)

Ketamine

Dextromethorphan

Dissociative Agents

Distort perceptions of sight and sound and produce feeling of being “out of body” and detached from environment

General Characteristics

White crystalline powder that is readily soluble in water or alcohol

Snorted, smoked or ingested

Memory loss and depression may persist for as long as a year after a chronic user stop taking PCP

MOA

Blocks NMDA-type glutamate receptors in cortex and limbic structures (ion channels)

Clinical signs

Doses of 10 mg or more* causes changes in blood pressure, heart rate, and respiration, often accompanied by nausea, blurred vision, dizziness and decreased awareness of pain, uncoordinated movements, bizarre postures

General Characteristics

“Meth”, “Crystal meth”

Taken orally, IV or smoked in form referred to as “ice”.

MOA

Dopaminergic and adrenergic reuptake inhibitor.

Euphoria and excitement occurs via stimulation of mesolimbic reward pathway

                             -->  

                     Abuse & addiction

SHORT term administration (Spree)

Short-term repeated administration (“spree”) causes intense euphoria (“RUSH”), increases alertness, self-confidence and ability to concentrate.

Increase in sexual urge

Decrease in appetite.

CHRONIC Use

Drug craving

Weight loss

Depression

Tooth decay* (“meth mouth”) – this is a KEY FEATURE!!

Neurotoxicity

Paranoia, hallucinations

MDMA

(Ecstasy, methylenedioxymethamphetamine)

Acute effects: tachycardia, dry mouth, jaw clenching* (Bruxism), muscle aches (higher doses effects include visual hallucinations, hyperthermia and panic attacks)

Confusion, drug craving, depression, sleep problems and severe anxiety

In HIGH doses, can interfere with the body’s ability to regulate body temperature*** (resulting in liver, kidney and CV system failure)***

Interaction with m receptors produces supraspinal and spinal analgesia, euphoria, sedation, respiratory depression and physical dependence.

Increase in pain threshold.

Decrease emotional reactivity to pain.

Euphoria results in development of psychological and physical dependence.

Tolerance occurs with repeated administration.

Abstinent withdrawal – autonomic hyperexcitability, muscle spasms, lacrimation, temor, diarrhea.

        -follows discontinuation of opioid-peaks at 48-72 h.

Precipitated withdrawal – induced by administration of opioid antagonist.

indicated for treatment of opioid withdrawal. Short-term detoxification (30 days) or long-term detoxification (180 days).

Ingested either alone or in combination with alcohol or other drugs.

Hypotension, memory impairment, dizziness, G.I irritation.

Long term use causes physical dependence.

Withdrawal symptoms may be delayed-hallucinations and seizures. – you want to take then off the Benzo SLOWLY!! You can get tremors, chest pain, if you take them off too quickly!!

Abstinence symptoms (anxiety, insomnia and irritability) will persist for several weeks.

“date rape drug”. – this starts its effect within 30 minutes and lasts for 8 hours and induces severe anterograde amnesia!!

Z-bars, Zandy bars, football, Zannies.

Can also cause anterograde amnesia

Chlordiazepoxide

Lorazepam

Benzodiazepine Withdrawal/Detoxification treated with chlordiazepoxide or lorazepam tapered over 5-7 days.