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CLINICAL TOXICOLOGY > CNS Depressants > Flashcards

CNS Depressants Flashcards

1
Q

Are CNS depressant sympatholytic or sympathomimetic

A

Sympatholytic

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2
Q

Most widely used substance of abuse

A

Alcohol

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3
Q

Medical uses of ethanol

A

Relief long lasting pain
Methyl alcohol and ethylene glycol poisoning
Disinfectant or antiseptic
Solvent

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4
Q

How is alcohol used to treat long lasting pain

A

Epidural, subarachnoid and lumbar paravertebral injections of ethanol destroys sympathetic ganglia and produce vasodilation and relieve pain

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5
Q

Which enzymes metabolize alcohol

A

Alcohol dehydrogenase
Aldehyde dehydrogenase
Mixed function microsomal oxidase (Cytochrome p450 2E1) or Microsomal Ethanol Oxidising Systems (MEOS)

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6
Q

Explain the biphasic activity of ethanol

A

Preferential suppression of inhibitory neurons followed by
Global inhibition of all CNS Neurons

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7
Q

Which receptors or pathways does alcohol affect

A

Enhance GABA and Glycine inhibition
Inhibit VG Ça channels
Activates K channels
Inhibits ionotropic Glutamate receptors
Inhibits adenosine transport

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8
Q

Effects of alcohol diuresis

A

Dehydration
Thirst
Lightheadedness

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9
Q

How does alcohol trigger an inflammatory response

A

Direct toxicity of acetaldehyde and alcohol on neurons

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10
Q

Effects of alcohol on glucose metabolism

A

Causes hypoglycemia by inhibiting gluconeogenesis

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11
Q

Effects of alcohol on vascular smooth muscle

A

Alcohol and acetaldehyde causes vasodilation

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12
Q

Effects of alcohol on gastric mucosa

A

Irritates lining of stomach and stimulates acid secretion

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13
Q

Why is acetaminophen avoided in managing alcohol abuse

A

It can exacerbate hepatotoxicity

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14
Q

Which drugs are used to alleviate acute symptoms of alcohol withdrawal

A

Benzodiazepines
Propranolol
Clonidine

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15
Q

Drugs to reduce alcohol craving

A

Naltrexone
Nalmefene
Baclofen
Acamprosate

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16
Q

Drugs to maintain remission in alcoholism

A

Topiramate
Acamprosate

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17
Q

Which fluid is used to replace potassium in hospitalized alcoholics

A

Ringers lactate

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18
Q

Which antacids are preferred to manage stomach upset in alcoholics

A

Aluminium based antacids are preferred over magnesium based antacids

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19
Q

Mild to moderate symptoms of alcohol withdrawal

A

Sweats
Tachycardia
Tremors
Insomnia
Anxiety
Psychomotor agitation

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20
Q

Severe symptoms of alcohol withdrawal

A

Generalised tonic clonic seizures
Delirium tremens
Hallucinations

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21
Q

Which receptors mediate alcohol withdrawal symptoms

A

GABA receptors
NMDA receptors

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22
Q

Which benzodiazepines are preferred in alcohol withdrawal

A

Longer acting ones
Chlordiazepoxide
Clorazepate
Diazepam

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23
Q

Why are longer acting benzodiazepines preferred in alcohol withdrawal

A

Easier weaning because they usually self taper on metabolism and excretion, leading to less fluctuations in plasma drug levels
They cause fewer rebours effects and withdrawal seizures

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24
Q

When are short acting benzodiazepines used in alcohol withdrawal

A

For alcoholics with liver disease and the elderly

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25
Q

Examples of short acting benzodiazepines

A

Lorazepam
Oxazepam
Temazepam

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26
Q

Role of thiamine and other vitamins in managing alcoholism

A

To increase glucose utilization by the brain

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27
Q

Role of antipsychotics in alcoholism management

A

To manage hallucinations and severe agitation

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28
Q

Examples of antipsychotics used in alcohol withdrawal

A

Haloperidol
Quetiapine

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29
Q

Role of baclofen in alcohol withdrawal

A

GABAb receptor agonist
Skeletal muscle relaxant
Antispasmodic

30
Q

Role of clonidine in managing alcohol withdrawal

A

alpha 2 agonist
Inhibits exaggerated neurotransmitter release

31
Q

Role of propranolol in alcohol withdrawal

A

Blocks effects of excessive sympathetic activity

32
Q

Name some agents whose metabolism is inhibited by disulfiram

A

Phenytoin
Oral anticoagulants
Isoniazid

33
Q

Drugs that can inhibit aldehyde dehydrogenase

A

Metronidazole
Cefotetan
Trimethoprim
Disulfiram

34
Q

Why is the combination of naltrexone and disulfiram avoided

A

Both are hepatotoxic

35
Q

Acamprosate is avoided in which patients

A

Patients with severe renal impairment

36
Q

Common adverse effects of Acamprosate

A

GIT effects - nausea, vomiting, diarrhea
Rash

37
Q

Does Acamprosate participate in any drug drug interactions

A

No

38
Q

Benefits of nalmefene in alcohol withdrawal

A

Longer duration of action
No dose dependent hepatotoxicity
Higher affinity for mu and kappa opioid receptors

39
Q

Role of gabapentin in alcoholism

A

Treat epileptic seizures and neuropathic pain

40
Q

Role of varenicline in alcohol withdrawal

A

Reduces alcohol consumption
Also used for smoking cessation

41
Q

What type of receptors are opioid receptors

A

GPCRs
Coupled t Gi and inhibit adenylyl cyclase

42
Q

Effect of mu receptors on dopamine

A

Located on inhibit GABA neurons which cause disinhibition of dopamine neurons

43
Q

Effects of Mu receptor activation

A

Euphoria
Dependence
Analgesia
Sedation
Depression

44
Q

Effect of kappa receptor activation

A

Expressed on and inhibit dopamine neurons causing dysphoria

45
Q

Oral bioavailability of tramadol

A

High oral bioavailability
Averaging 70% irrespective of food

46
Q

Mechanism of tramadol

A

Low affinity to mu receptors
Increases serotonin release
Inhibits serotonin and noradrenaline reuptake

47
Q

Symptoms of opioid withdrawal

A

Piloerection
Dysphoria
Lacrimation
Mydriasis
Restlessness
Abdominal cramps

48
Q

Uses of clonidine in opioid withdrawal

A

Attenuate the symptoms of anxiety, hypertension, piloerection, tachycardia and chills

49
Q

Role of methadone in opioid withdrawal

A

long acting mu-opioid agonist that suppresses withdrawal symptoms and controls the craving for opioids in maintenance therapy

50
Q

Why is methadone a good choice for opioid withdrawal

A

It has less likelihood of inducing withdrawal symptoms due to its long duration of action

51
Q

Drugs used to maintain remission in opioid withdrawal

A

Naltrexone
Nalmefene

52
Q

Nalmefene or Naltrexone be used at least …… days after abstinence to avoid inducing acute withdrawal.

A

Seven

53
Q

Advantages of Nalmefene relative to naltrexone

A

Longer half life
No hepatotoxicity
Greater oral bioavailability

54
Q

Mechanism of action of buprenorphine

A

Partial mu receptor agonist

55
Q

Role of buprenorphine in opioid use disorder

A

Reduces craving whiles blocking or blunting the euphoric effects of full agonist

56
Q

How long should benzodiazepines be prescribed to avoid dependence

A

1-2 weeks

57
Q

How long does it take to develop dependence when one is on benzodiazepines

A

3-4 weeks

58
Q

For which effects are benzodiazepines mostly abused

A

Euphoric effects

59
Q

Action of benzodiazepines

A

Sedatives
Anxiolytic
Anticonvulsant

60
Q

Examples of ultrashort scaring benzodiazepines

A

Midazolam
Zolpidem

61
Q

Short acting benzodiazepines

A

Lorazepam
Oxazepam
Temazepam

62
Q

Long acting benzodiazepines

A

Chlordiazepoxide
Flurazepam
Diazepam
Clonazepam
Clorazepate

63
Q

Medium acting benzodiazepines

A

Alprazolam
Nitrazepam

64
Q

Symptoms of benzodiazepines withdrawal

A

Insomnia
Restlessness, agitation, paranoia
Severe headaches
Manic disorders
Perceptual disorders
Hallucinations
Seizures
Sweating, muscle cramps, twitches

65
Q

Anticonvulsants used in benzodiazepines withdrawal

A

Carbamazepine
Pregabalin

66
Q

Antidote for benzodiazepines withdrawal

A

Flumazenil

67
Q

Symptoms of barbiturate toxicity

A

Respiratory depression
Hypothermia
Sweating
Ataxia
Generalised seizures
Vertigo
Slurred speech
Altered consciousness
Insomnia
Anxiety
Tremors

68
Q

Effects for which benzodiazepines are abused

A

Euphoria
Relaxation
Drowsiness
Disinhibition

69
Q

Symptoms of barbiturates withdrawal

A

Grand mal seizures
Increased temperature
Shaky hands
Tachycardia
Tachypnea
Insomnia
Hyperthermia

70
Q

Examples of barbiturates

A

Amobarbital- Amytal
Secobarbital- Seconal
Phenobarbital
Butalbital
Thiopental

CLINICAL TOXICOLOGY (14 decks)

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