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Pharm 2 Part 1 > Lecture 3: Alcohol and its Tx and Muscle Relaxants > Flashcards

Lecture 3: Alcohol and its Tx and Muscle Relaxants Flashcards

1
Q

How does Alcohol depress synaptic transmission in the CNS?

A

Interacts w/GABAa Receptor. Increases Cl- influx, and augments GABA Transmission

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2
Q

What does Long-term use do to GABA receptors?

A

Down-regulate GABA receptors by DECREASING SYNTHESIS

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3
Q

Alcohol can also inhibit the effect of what Excitatory AA?

a. On what receptor?
b. What is this receptor involved in?
c. What does long-term use of alcohol do to this receptor?

A
  1. Glutamate
    a. NMDA receptor
    b. Learning and Memory. also in creating SEIZURE Activity
    c. Up-Regulates the NMDA Receptors
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4
Q

At low doses, what does alcohol do?

A

Inhibits Inhibitory pathways (DISINHIBITION)…so it seems to be a stimulant at first.

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5
Q

What does alcohol do to sleep?

A

Decreases time spent in REM sleep and DECREASES OVERALL QUALITY of SLEEP.

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6
Q

Alcohol: Pharmacokinetics

  1. How is it absorbed?
  2. What can it cross?
  3. Most alcohol is metabolized by what?
  4. Alcohol Oxidation follows what Order kinetics?
    a. Typical amt metabolized?
A
  1. Rapidly and COMPLETELY from the stomach and Small Intestine. Peak blood levels w/in 30-90 min after the last drink
  2. BBB and Placenta
  3. Alcohol Dehydrogenase in the LIVER
  4. ZERO ORDER KINETICS
    a. 7-10 g of 100% alcohol per hour.
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7
Q

Alcohol: Pharmacokinetics (2)

  1. Chronic Alcohol Consumption INDUCES what?
  2. What is PHARMACODYNAMIC TOLERANCE?
  3. In chronic drinkers, NADP+ decreases availability of what?
    a. Which is used for what purpose?
    b. What does this increase?
    c. What do we think this contributes to?
  4. What does DISULFIRAM do?
A
  1. CYP2E1
  2. Effects at a given blood level of alcohol are LESS in chronic Drinkers
  3. of NADPH
    a. to Regenerate Reduced GLUTATHIONE
    b. Oxidative Stress
    c. Liver Damage
  4. Inhibits Aldehyde Dehydrogenase. Causes Very Unpleasant and Dangerous Effects with Alcohol
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8
Q

Alcohol: Pharmacokinetics (3)

  1. What normal OTC medicine can cause Heptaotoxicity in Alcoholics?
    a. Why?
  2. Chronic Alcohol consumption may do what to the METABOLISM of DRUGS?
  3. Acute Alcohol Consumption may do what?
A
  1. Acetaminophen (Tylenol)
    a. CYP2E1 is INDUCED
  2. May INCREASE the METABOLISM of DRUGS
  3. COMPETE for metabolism and Inhibit the breakdown of some drugs
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9
Q

Effects of Alcohol

  1. CNS: What does it do at LOW Concentrations? (4)
  2. W/INCREASED Dose, what happens next?
    a. What is this called?
  3. In Chronic Drinkers, what levels of alcohol are needed to produce the same effect as in Occasional Drinkers?
  4. What does Ethanol act as?
    a. What does Large amts of it do to your BT?
    b. What does it do to the uterus?
  5. What does it do in the kidney?
A
  1. Dis-inhibition, Decreased Anxiety, Mild Euphoria, and Sedation
  2. Motor Function and Judgement are Impaired, Speech Slurs, and Ataxia can occur.
    a. Intoxication
  3. Much higher levels. Due to Increased Metabolism, Pharmacodynamic Tolerance Develops (maybe due to down-regulation of GABA receptors, and up-regulation of NMDA Receptors)
  4. VASODILATOR
    a. Cause HYPOTHERMIA
    b. Relaxes it, and has been used via IV to prevent premature labor.
  5. Decreases ADH, thus has a DIURETIC EFFECT.
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10
Q

Alcohol Toxicity

  1. When Blood levels increase from 200 to 500 mg/dL, what effects occur? (5)
  2. How do you treat SEVERE Intoxication?
  3. What can it do to metabolism?
  4. Why can Hypothermia result?
A
  1. Coma, Emesis, Stupor, Respiratory Depression, and even death can occur.
  2. Manage Respiratory Depression and prevent aspiration of vomit
  3. Cause Metabolic and Electrolyte Disturbances. treat with PHENYTOIN if Seizures happen
  4. Cuz of Cutaneous Vasodilation…causes flushing of the skin and a feeling of warmth.
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11
Q

What do we think Hangovers are?

A

Buildup of ACETALDEHYDE, Dehydration, start of Withdrawal, and accumulation of mild toxic compounds associated with Alcoholic Beverages

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12
Q

Effects of Chronic Alcohol Consumption

  1. Malnutrition: Why?
    a. 2 Major deficiencies?
  2. Gastritis and Pancreatitis
    a. Why?
    b. What does Gastritis cause?
    c. What does alcohol disrupt in the stomach? What does this lead to?
A
  1. It has a LOT of CALORIES
    a. Folate and Thiamine
  2. a. Direct damage to pancreatic cells, and stimulates Acid production, causing major Erosive Gastritis, and Malabsorption
    b. Malabsorption of Water-Soluble Vitamins
    c. Gastric Mucosa. Gastritis and Esophageal Reflux…we see Lesions of ESOPHAGUS and DUODENUM quite often.
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13
Q

Effects of Chronic Alcohol Consumption (2)

  1. Hepatotoxicity
    a. Alcohol metabolism does what to GLUTATHIONE? What does this cause?

b. Acetaldehyde increases what?
c. What develops after prolonged heavy drinking? Followed by what? This can lead to what?

d. Alcohol Hepatitis can occur. Coexistence of what will increase damage of liver?
i. What will most likely occur?

A
  1. a. Decreases it. (normally gets rid of Free Radicals…so increased oxidation); Oxidative stress and tissue damage.
    b. Lipid Peroxidation. Damages Mitochondrial and cell membranes (hepatocytes fill w/protein, fat, and water)
    c. Fatty Liver; Fibrosis; Collagen Deposit which leads to CIRRHOSIS
    d. Hep B or C
    i. Liver Cancer in patients w/cirrhosis and Hep C in about 10 years after alcohol consumption is stopped. (why? Cuz the liver tries to heal itself)
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14
Q

Effects of Chronic Alcohol Consumption (3)

  1. Cardiovascular Effects
    a. Small amts of alcohol will do what?
    b. Chronic heavy drinking may do what?
  2. What can Binges do?
  3. CARDIOMYOPATHY may develop due to what?
  4. Heavy Alcohol Consumption contributes to what?
  5. There is an increased risk of what occurring?
A
  1. a. (1-3 drinks a day) can reduce CHD by increasing HDL
    b. Heart damage
  2. Severe INCREASES in BP and can cause Arrhythmias.
  3. direct toxic effects of Acetaldehyde on the heart.
  4. HYPERTENSION
  5. STROKE in peeps who drink more than 4-6 drinks per day, or after binge drinking.
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15
Q

Effects of Chronic Alcohol Consumption (4)

  1. Teratogenicity
    a. FAS: Characterized by what?
  2. Carcinogenicity: of what?
  3. Blood?
  4. Sexual Function?
  5. Immune System?
  6. Korakoff’s Psychosis?
    a. Wernicke Encephalopathy?
    b. These 2 are a result of what?
  7. What 3 other things can happen?
A
  1. Microcephaly, mental retardation, poor coordination, flattened face, joint abnormalities, heart defects, impaired immune system.
  2. Tobacco Products
  3. Mild Anemia (due to Folic Acid Deficiency), Iron Deficiency, and GI Bleeding
  4. Testicular atrophy, impotence, gynecomastia
  5. Respiratory infections common due to impaired immune function in lung
  6. chronic memory loss
    a. paralysis of eye muscles, ataxia, confusion
    b. Nutritional deficiencies, esp Thiamine
  7. Peripheral Neuropathy, Skeletal Muscle Atrophy, and Hypothermia
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16
Q

Tolerance and Dependence

  1. Why does it develop?
  2. Severe Withdrawal syndrome due to what?
  3. Cross-Tolerance to effects of what 3 things?
    a. Lethal dose?
A
  1. Pharmacodynamic (alcohol) and Pharmacokinetic (increased metabolism)
  2. Pharmacodynamic tolerance
  3. Barbiturates, Benzodiazepines, General anesthetics
    a. Does not change
17
Q

Alcoholism

  1. Use of alcohol in peeps w/a predisposition to alcoholsim causes what to happen?
A
  1. Increase release of B-endorphins in Dopamine Reward Pathway (goes from VTA to Nucleus Accumbens and Prefrontal Cortex)
18
Q

Alcohol Withdrawal

  1. When do symptoms start?
  2. MILD WITHDRAWAL: Includes what symptoms?
  3. SEVERE WITHDRAWAL includes what symptoms?
A
  1. 6-24 hrs and can last about 5 days
  2. Anxiety, irritability, insomnia, nightmares, nausea, tachycardia, and palpitations…can last 1-2 days
  3. Anxiety, fear, hallucinations, delirium and tremors, tonic-clonic seizures, arrhythmias, increased BP
19
Q

Tx of Alcohol Withdrawal

  1. Main goal is to prevent what 3 things?
  2. What drugs can be used to TAPER the Withdrawal?
    a. What is used if there’s liver damage?
  3. What can be used to treat Hallucinations or Aggression in an ER setting?
A
  1. Seizures, DTs, and Arrhythmias
  2. LONG-ACTING Benzos (DC)
    a. Shorter acting Benzo like OXAZEPAM
  3. Antipsychotics (like HALOPERIDOL)
20
Q

Tx of Alcoholism: DISULFIRAM

  1. What does it block?
  2. What does ACETALDEHYDE produce? (4)
  3. Action time?
  4. What other drugs should not be combined with alcohol that have similar effects as Disulfiram?
  5. What does Disulfiram inhibit?
  6. Is it recommended?
A
  1. ALDEHYDE DEHYDROGENASE
  2. Flushing, Intense and throbbing headaches, Nausea, Confusion…all of this can be SEVERE and lead to vomit, sweating, chest pain, hypotension, etc.
  3. Long. DONT drink 3-4 days after taking it.
  4. Metronidazole, some Cephalosporins, and Oral Hypoglycemic Agents
  5. p-450, so can interfere w/Phenytoin, chlordiazepoxide, barbituarates, and warfarin metabolism
  6. NO! ITS DANGEROUS!
21
Q

Tx of Alcoholism: NALTREXONE

  1. What is it?
  2. How can it be given?
  3. What does it do?
  4. Effect on RELAPSE?
  5. Major SIDE EFECT?
  6. In LARGE DOSES, what can it do?
A
  1. Opioid Receptor Antagonist
  2. Orally or once a month by depot injection
  3. BLOCKS ability of Alcohol to stimulate REWARD PATHWAY
  4. DECREASES RATE of RELAPSE by 50%
  5. NAUSEA…more common in women.
  6. cause LIVER DAMAGE. (CI in pts w/liver disease, hepatitis, or liver failure)
22
Q

Tx of Alcoholism: ACAMPROSATE

  1. What is it?
  2. What does it do?
  3. It can be VERY EFFECTIVE if used in conjunction w/what treatment?
  4. Side effects?
  5. How does the body get rid of it?
  6. Liver toxicity?
A
  1. Structural analogue of GABA
  2. Restores normal balance of GABA and GLUTAMATE Transmission
  3. Psychosocial treatment
  4. None (no anxiolytic, antidepressant, or psychotropic effects)..So NO ABUSE POTENTIAL
  5. Kidneys
  6. NONE
23
Q

Tx of Alcoholism: Other Drugs

  1. Topiramate
    a. Type of drug?
    b. What does it seem to do?
  2. Gabapentin
    a. What is it?
    b. What does it seem to do?
A
  1. a. Anticonvulsant
    b. decrease craving and help recovering alcoholics not return to alcohol.
  2. a. Anticonvulsant
    b. Decreases alcohol use.
24
Q

Muscle Relaxants

  1. What do they relieve?
A

Spastic Muscle disorders due to a LOSS of SUPRASPINAL CONTROL and heightened excitability of motor systems.

25
Q

Central Acting Muscle Relaxant Drugs: Diazepam

  1. What does it act on?
  2. High doses can result in what?
  3. May be used for SPASMS associated with what?
A
  1. GABAa Receptors in Spinal Cord
  2. Sedation (Doses high enough to reduce spasticity)
  3. with LOCAL MUSCLE TRAUMA
26
Q

Central Acting Muscle Relaxant Drugs: BACLOFEN

  1. What receptor does it act on?
    a. What does this do?
  2. It could reduce pain. Why?
  3. How do you take it?
    a. Half life in blood?
  4. What other administration could be used?
    a. Why would we use this method?
    b. Bad things that could happen with this method?
  5. Side effects?
A
  1. Agonist: GABAb receptors
    a. HYPERPOLARIZATION. Inhibits release of EXCITATORY transmitters from PRESYNAPTIC TERMINALS in brain and spinal cord.
  2. Inhibits release of Substance P from the Spinal Cord
  3. Oral.
    a. 3-4 hrs
  4. INTRATHECAL ADMINISTRATION
    a. Helps to better control pain, spasticity, and decreases peripheral symptoms
    b. coma could happen
  5. DROWSINESS, MEMORY LOSS and CONFUSION. May increase seizures in epileptics
27
Q

Central Acting Muscle Relaxant Drugs: TIZANIDINE

  1. Analogue of what drug?
  2. Acts on what receptors?
  3. Used to do what?
  4. May cause what?
  5. HYPOTENSION can occur if combined with what drugs?
  6. Main Side effects? (5)
A
  1. CLONIDINE
  2. Agonist at A2 Receptors
  3. REDUCE CHRONIC MUSCLE SPASTICITY from spinal chord injury
  4. Significant SEDATION
  5. antihypertensive drugs
  6. drowsiness, dry mouth, muscle weakness, hypotension, sedation
28
Q

Sedating Muscle Relaxants

  1. Where do they work?
  2. Not really effective. Include what 6 drugs?
A
  1. at brain stem…act as sedatives
  2. CCCMMO
    a. CARISOPRODOL
    b. CYCLOBENZAPRINE
    c. CHLORZOXAZONE
    d. METAXALONE
    e. METHOCARBAMOL
    f. ORPHENADRINE
29
Q

Sedating Muscle Relaxants: CARISOPRODAL (SOMA)

  1. Type of drug?
  2. Action on muscle?
  3. May alter what?
  4. Metabolized to what?
    a. This acts like what?
  5. Problems with it?
  6. Chronic use INDUCES what?
A
  1. SEDATIVE
  2. No direct action
  3. PERCEPTION OF PAIN
  4. MEPROBAMATE
    a. Like Barbiturates
  5. SIGNIFICANT DRUG ABUSE
    (Dont give to a recovering addict or alcoholic)
  6. HEPATIC MICROSOMAL ENZYMES
30
Q

Sedating Muscle Relaxants: CYCLOBENZAPRINE

  1. Similar to what?
  2. Type of Activity?
  3. Used for TEMPORARY RELIEF of what?
  4. Problems?
A
  1. Tricyclic Antidepressants
  2. ANTICHOLINERGIC ACTIVITY
  3. ACUTE MUSCLE SPASMS from Trauma or Sprain
  4. very SEDATING; Can produce CONFUSION and TRANSIENT VISUAL HALLUCINATIONS
31
Q

Dantrolene

  1. What does it do?
  2. Used to treat what?
  3. What drugs can produce a similar reaction?
A
  1. Affects Excitation-Contraction coupling in muscle. Does this by INTERFERING with release of CALCIUM from SR
  2. MALIGNANT HYPERTHERMIA (induced by general anesthetic w/neuromuscular blocking agents) Happens in peeps w/a genetic impairment in ability to sequester calcium in SR.
  3. ANTISPYCHOTIC DRUGS cause a SIMILAR RxN (NEUROLEPTIC MALIGNANT SYNDROME…which is also treated w/dantrolene)
32
Q

Botulinum Toxin

  1. What does it do?
  2. Large concentrations do what?
  3. How is it administered?
A
  1. Blocks release of ACH from presynaptic nerve terminals
  2. cause local muscle paralysis in small amts
  3. INJECTED to CONTROL LOCAL MUSCLE SPASMS…often due to neurologic injury or stroke. (Promoted to remove wrinkles and lines)

Pharm 2 Part 1 (6 decks)

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