Comprehensive Guide to Barbiturates, Benzodiazepines, and CNS Depressants in Pharmacology

What are barbiturates?

Depressant drugs that induce sedation and sleep.

Who discovered barbiturates?

Adolf von Baeyer.

What is the mechanism of action of barbiturates?

They slow down neural activity in the central nervous system and disinhibit the cerebral cortex

What are some characteristics of barbiturates?

Relatively tasteless and ordorless, reliably induces sleep

What are barbiutrates prescribed for?

Historically for insomnia, but now epilepsy and surgical anesthesia

What is the elimination half-life of barbiturates?

10-40 hours up to 50-120 hours

What are the acute effects of barbiturates at low doses?

Relaxation and a sense of euphoria.

What are the therapeutic doses of barbiturates used for?

Sedation and drowsiness.

What are the effects of barbituates at high doses?

Hypnotic (sleep-inducing)

What is the overdose potential of barbiturates?

The most serious risk, either from taking too high a dose or taking it in combination with alcohol

What is is the biggest risk of barbiturates?

Excessive dose produces an inhibition of the respiratory control centers in the brain

What are the effects if you combine barbiturates with acohol?

Synergistic effect (combined result is greater than the sum of the effects of each drug alone)

What are common withdrawal symptoms from barbiturates?

Tremors, nausea, vomiting, confusion, convulsions, hallucinations; most dangerous and distressing type of drug withdrawal; closely resemples withdrawal after chronic alcohol abuse

What is the effect of benzodiazepines?

They have a selective effect on anxiety without general sedation; also slow onset, no "rush; tranquilizing rather than sedative effects

What is a major adverse effect of benzodiazepines?

They can produce drug-induced dementia in elederly patients

What is tolerance to benzodiazepines like?

Little problem with tolerance when taken to reduce anxiety, but there is distinct tolerance

What neurotransmitter do benzodiazepines primarily affect?

GABA (heightens its inhibitory effect on CNS)

What is a key characteristic of benzodiazepines?

They are absorbed slowly into the bloodstream from small intestine and don't affect the respiratory centers in the brain

What are common withdrawal symptoms from benzodiazepines?

Increased anxiety, insomnia, restlessness, agitation (gone in 1-4 weeks).

What is the overdose potential of benzodiazepines?

Almost impossible due to lack of impact on respiratory system.

What are inhalants?

Substances that inhibit CNS and produce intoxication effects (also slow down brain waves)

What are common effects of inhalants?

Euphoria, dizziness, slurred speech, hallucinations, giddiness, recklessness/omnipotence; hits fast, toxic effect on organs

What is the toxicity concern with inhalants?

Concentration of exposure can be 50 to 100 times greater than safe levels/allowable in industry exposure; 13 times greater risk of birth defects for pregnant women

What are the withdrawal symptoms of inhalants?

Rstlessness, irritability, anxiety

What are beta blockers used for?

Control of high blood pressure and anxiety-producing events.

What is the effect of beta blockers on the heart?

They slow heart rate, relax pressure on blood vessel walls, and decrease force of heart contraction.

What are some common drugs related to benzodiazepines?

Diazepam, Xanax, Rohypnol, Valium

What is the mechanism of action of beta blockers?

They block beta-adrenergic receptors.

What is a characteristic of barbiturates regarding sleep?

They suppress REM sleep.

What is the mechanism of action of zolpidem (Ambien)?

It's a sedative-hypnotic that binds to a subtype of GABA receptor (but isn't a benzodiazepine)

What are the effects of zolpidem?

Strong but transient sedative effects with little to no muscle relaxation; used for treatment of insomnia

What is GHB?

Gamma-hydroxybutyrate, a colorless, odorless, virtually tasteless substance that produces an "out-of-body" high

What is the primary use of buspirone?

It relieves anxiety (anxiolytic) by acting on a subclass of serotonin receptors

What are the pros of buspirone?

There are no cross-tolerance effects with alcohol, no withdrawal, no impairment in motor skills

What is nitrous oxide commonly known as?

Laughing gas (used by dentists as anesthetic)

What are the risks associated with nitrous oxide?

It can lead to hypoxia.

What is methaqualone classified as?

A nonbarbiturate depressant/sedative-hypnotic drug; used to be a sleeping pill, now a Schedule I Controlled Substance and "date-rape" drug

What is meprobamate known for?

It was the first anxiolytic drug developed and it genuinely worked

Cons of meprobomate

Diminished motor reflexes and made people drowsy; produced depedence at more than twice the normal recommended daily dose; Classified as schedule IV controlled substance

What is diazepam commonly known as?

Valium (for the treatment of anxiety)

What is the effect of toluene inhalation?

It can cause reduction in short-term memory, anemia, and hearing loss.

What is the primary use of amobarbital?

It is a sedative-hypnotic drug.

What is the brand name of alprazolam?

Xanax (shorter acting oral benzodiazepine for sleeping problems)

What is the effect of hexane inhalation?

It is associated with peripheral nerve damage, leading to muscular weakness and atrophy

What is ether used for?

It was used as an anodyne for intestinal cramps and toothaches and resembled intoxication

What is Rohypnol?

Long-acting benzodiazepine that is highly synergistic with alcohol and implicated in DFSA cases

What is the strength comparison of Rohypnol to Valium?

Rohypnol is ten times stronger than Valium

What are the active ingredients in OTC sleep aids like diphenhydramine hydrochloride, doxylamine succinate, and diphenhydramine citrate?

CNS depressants.

What neurotransmitters should be known in pharmacology?

GABA, serotonin, dopamine.

What is hypoxia?

A deficiency in oxygen intake.

What age group tends to use inhalants?

Young children, typically ages 11-13.

What was the purpose of the Pure Food and Drug Act of 1906?

To ensure food and drugs in the U.S. were inspected for purity and consistency; all active ingredients need to be clearly, accurately identified on label

What are the phases of the FDA drug approval process?

Phase 1: 10-100 healthy volunteers; Phase 2: 100-500 patients with condition; Phase 3: 1,000-3,000 patients monitored, New Drug Application submitted to FDA after 3+ years; Phase 4: post-marketing monitoring.

What was the Federal Food, Drug, and Cosmetic Act of 1938 intended to do?

Basic food and drug regulatory law that required companies to demonstrate drug safety before marketing commercially and required that all ingredients be accurately identified

How long do drug patents last?

They last for a fixed duration of 20 years.

What is bioequivalence?

It refers to two drugs having the same pharmacological and physiological effects.

What is a brand name?

The registered name used by the original company under the patent; they tend to continue marketing the drug under its brand name even when the patent expires

What are generic drugs?

Forms of a drug that are manufactured and sold to the public after the 20 year patent is up; tend to be much less expensive; bioequivalent, but different bioavailability

What is aspirin used for?

It is used for mild to moderate pain, anti-inflammatory, antipyretic, and has anticlotting effects.

What is acetaminophen commonly known as?

Tylenol; only pain relieving; equivalent effect on pain as aspirin, bit without the side effects

What is the primary use of ibuprofen?

It reduces pain, inflammation, and elevated temperature (Advil, Motrin, Buprin)

What is naproxen known for?

It is an anti-inflammatory and antipyretic with a longer duration of action than other OTC analgesics (8-12 hours)(Aleve)

What population should avoid pseudoephedrine?

Young children under age 4.

How are dietary supplements treated differently from drugs?

They don't need to be tested for safety or effectiveness but must be free of contaminants and labels must accurately reflect the contents (aren't classified as drugs)

What was the Kefauver-Harris Amendment of 1962 intended to do?

It required drug companies to prove new drugs were effective as well as safe to ensure that all drugs (both prescription and nonprescription) sold in the U.S. were bpoth safe and effective; GRAHL, GRAS, GRAE

What is an IND?

An Investigational New Drug application submitted to the FDA; sent to FDA after preliminary studies and drug has been determined to be safe with animals

What types of diseases have expedited drug treatments?

AIDS, infections associated with kidney transplants, Alzheimer's disease, Parkinson's disease, and some advanced cancers.

What are NSAIDs and what do they treat?

Nonsteroidal anti-inflammatory drugs that reduce pain and swelling caused by injury or disease.

What are prostaglandins?

A group of hormone-like chemicals produced by body cells when injured, encourage inflammation and fever; blocked by many OTC analgesics

How much of the FDA approval process is designated for drug regulation?

1/3 of the entire FDA budget.

How many prescription errors occur annually for the elderly population?

500,000.

What class of drugs contains opioid dextromethorphan?

Cough-and-cold remedies.

What is robo-tripping?

Getting high off of/abusing dextromethorphan (cough-and-cold rememdy).

What is Medicare Part D?

Federal legislation regarding prescription drug reimbursement for Medicare beneficiaries; optional, private insurance that covers prescription drugs for Medicare beneficiaries

What does GRAHL stand for?

Generally regarded as honestly labeled.

What does GRAS stand for?

Generally regarded as safe.

What does GRAE stand for?

Generally regarded as effective.

What is OTC?

Over-the-counter drugs available without a prescription.

What is an antipyretic?

A medication used to reduce, prevent, or relieve fever.

What is an antitussive?

A medication that suppresses or relieves coughing.

What is an analgesic?

A medication used to manage and relieve pain.

What is an antihistamine?

A medication used to treat allergy symptoms.

Who can take aspirin safely?

People age 20 and older.

What is Reyes Syndrome?

A rare but dangerous childhood disorder associated with ASA-type analgesic drugs (Aspririn); marked by lethargy, nausea, sever vomiting, disorientation, and coma

What label must dietary supplements have?

Must accurately reflect contents and state that claims have not been evaluated by the FDA.

What is the concordance rate for schizophrenia in monozygotic twins?

48%.

What is the biomedical model of mental illness?

The position that mental disorders are caused by abnormal biochemical processes in the brain.

What is the diathesis-stress model?

Mental disorders develop from a combination of pre-existing vulnerability and environmental stress.

What were the treatment options for schizophrenia prior to the 1950s?

Heavy administration of barbiturates and neurosurgical interventions.

What is Tardive dyskinesia?

A serious side effect affecting schizophrenia patients treated with first-generation antipsychotic drugs; characterized by jerky movements of face and lips, unsteadienss in walking, and rocking when seated

What are the three types of symptoms that characterize schizophrenia?

Positive symptoms, negative symptoms, and cognitive symptoms.

What are positive symptoms of schizophrenia?

Addition to a person's experience (distortion of reality); psychotic behaviors not typically seen in healthy people

What are negative symptoms of schizophrenia?

Withdrawal or reduction in normal functioning; disruptions to normal emotions and behaviors

What are cognitive symptoms of schizophrenia?

Decline in mental processing, making it hard to lead a normal life; disordered thinking and memory issues

What is aripiprazole?

Brand name Abilify, a third-generation antipsychotic effective for schizophrenia and BPD without risk of Parkinson's side effects, tardive dyskinesia, agranulocytosis, weight gain, or diabetes; increases functioning of D2 receptors

What is meant by the term psychotrophic?

Another word for psychiatric drugs; moving the patient closer to a normal state of mind

What is Valproate?

A drug used for patients suffering from mania or bipolar disorder.

What is Clozaril?

A second-generation antipsychotic effective for many schizophrenia patients.

What is Risperdal?

A second-generation antipsychotic that can cause significant weight gain; not for elderly people; can also be used for BPD

What is meant by the term off-label?

Prescribing a medication for a purpose not FDA-approved.