Topic 5: Drugs that Affect the neurological system Flashcards
Barbiturates (No Antidotes)
a class of drugs used to induce sedation; chemical derivatives of barbituric acid
Barbiturates (No Antidotes) Phenobarbital (Luminol Sodium)
considered prototypical barbiturate; classified as a long-acting drug
Barbiturates (No Antidotes) Phenobarbital (Luminol Sodium) Mechanism of action
CNS depressants acts primarily on brainstem (‘reticular formation’)
- sedative and hypnotic effects are dose related
- act by reducing nerve impulses traveling to area of the brain (cerebral cortex)
- ability to inhibit nerve impulse transmission due in part to ability to potentiate the action of inhibitory neurotransmitter GABA, found in high concentration in CNS
- Barbiturates raise seizure threshold; can be used to treat seizures
Barbiturates (No Antidotes) Phenobarbital (Luminol Sodium) Indications
- prevention of generalized tonic-clonic seizures and fever-induced convulsion
- useful in Tx of hyperbilirubinemia in neonates
- rarely used today as a sedative and is no longer recommended to be used as a hypnotic drug
Indications for Barbiturates
All barbiturates have same sedative hypnotic effects but differ in their potency, time to onset of action, and duration of action. The various categories of barbiturates can be used to the following therapeutic purposes: ultrashort, short, intermediate, and long acting
Barbiturates (No Antidotes) Phenobarbital (Luminol Sodium) Contraindication
known drug allergy, pregnancy, significant respiratory difficulties, and severe kidney or liver disease. These drugs (barbs) must be used with caution in older adults due to their sedative properties and increased fall risk
Barbiturates (No Antidotes) Phenobarbital (Luminol Sodium) Adverse effects
low therapeutic index; long acting, adverse effects relate to the CNS and include drowsiness, lethargy, dizziness, hangover, and paradoxical restlessness or excitement. -Barbs deprive people of their REM sleep which can result in agitation. With most sedative drugs the risk of fall occurs so for older adults it can be suggested to take half of dose
Barbiturates (No Antidotes) Phenobarbital (Luminol Sodium) Assessment
- insomnia, any concerns voiced about sleep patterns or disorders, the time it takes to fall asleep, vitals, physical assessment, renal and liver, mental status, miscellaneous info about medical history, use of drugs etc.,
- evaluate cautions, contraindications, and drug interactions
- NOT to be used pregnant or lactating women- these drugs cross the placenta and breast-blood barriers posing a risk for respiratory depression in the fetus and neonate. If women take while pregnant baby will have withdrawal symptoms
Barbiturates (No Antidotes) Phenobarbital (Luminol Sodium) Patient teaching
advice about hangover effects to older patients, encourage to keep journal of sleep, avoid caffeine when trying to go to bed (avoid at least 6 hours before bedtime), keep drugs out of the reach of children, emphasize to take as required, educate about driving or operation of heavy machine while taking those drugs
Difference between sedatives and hypnotics
-Sedatives reduce nervousness, excitability, and irritability
without causing sleep, but a sedative can become a hypnotic if it is given in large enough doses.
-Hypnotics cause sleep and have a much more potent effect on the CNS than do sedatives
Phenobarbital is also used to treat?
status epilepticus (prolonged uncontrolled seizures). In extreme cases, patients may be intentionally overdosed to the extent of causing therapeutic phenobarbital or pentobarbital coma
Benzodiazpenes
a chemical category of drugs most frequently prescribed as anxiolytic (drugs used to reduce intensity of anxiety) drugs and less frequently as sedative-hypnotic agents
Benzodiazpenes Diazepam (Valium) - long acting Mechanism of action
Diazepam (Valium) - long acting
Mechanism of action: sedative and hypnotic action is related to ability to depress activity in CNS. Specifically the hypothalamic, thalamic, and limbic systems of the brain. Because research suggest they are GABA receptors or other adjacent receptors. GABA- primary inhibitory neurotransmitter of the brain and it serves to modulate CNS activity by inhibiting overstimulation
Benzodiazpenes Diazepam (Valium) Indications
treatment of anxiety, procedural sedation, and anesthesia adjunct, anticonvulsant therapy, and skeletal relaxation following orthopedic injury or surgery
Benzodiazpenes Diazepam (Valium) contraindication
drug allergy, narrow-angle glaucoma, and pregnancy
Benzodiazpenes Diazepam (Valium) Adverse effects
can be harmful if dose is mixed with alcohol, headache, drowsiness, paradoxical excitement or nervousness, dizziness, vertigo, cognitive impairment and lethargy. Fall hazard for older population, have comparatively less intense effects on the normal sleep cycle, ‘hangover’ effect is sometimes reported (daytime sleepiness), withdrawal symptoms like rebound insomnia. Amnesia, anorexia, sedation, lethargy, fatigue, confusion, drowsiness, dizziness, ataxia, headache, visual changes, hypotension, weight gain or loss, nausea, weakness
Benzodiazpenes Diazepam (Valium) Toxicity/management
when taken with alcohol, barbiturates, overdose causes somnolence, confusion, diminished reflexes, and coma. Treatment is the antidote Flumazenil
Benzodiazpenes Diazepam (Valium) Interactions
alcohol, opioids, muscle relaxants will cause intense CNS depressant, kava and valerian are herbal supplements that interact and can lead to CNS depression, grapefruit results in prolonged effect, increased effect and toxicity
Benzodiazpenes Diazepam (Valium) Assessment
vitals, identification of disorders or conditions that pose threat for caution or contraindications, monitor suicide, anemic, have history of substance/alcohol abuse, caution pregnant or lactating patients, renal functions or hepatic function studies to help prevent toxicity or complications, pay attention to drug interactions
Benzodiazpenes Diazepam (Valium) Patient teaching
advice about hangover effects to older patients, encourage to keep journal of sleep, avoid caffeine when trying to go to bed (avoid at least 6 hours before bedtime), keep drugs out of the reach of children, emphasize to take as required, educate about driving or operation of heavy machine while taking those drugs
Benzodiazpenes Midazolam (Versed) – short acting Mechanism of action
sedative and hypnotic action related to ability to depress activity in the CNS. Specifically the hypothalamic, thalamic, and limbic systems of the brain. Because research suggest they are GABA receptors or other adjacent receptors. GABA- primary inhibitory neurotransmitter of the brain and it serves to modulate CNS activity by inhibiting overstimulation
Benzodiazpenes Midazolam (Versed) Indication
commonly used preoperatively and for moderate sedation. It has the ability to cause amnesia and anxiolysis (reduced anxiety), as well as sedation
Benzodiazpenes Midazolam (Versed) contraindications
drug allergy, narrow-angle glaucoma, and pregnancy
Benzodiazpenes Midazolam (Versed) adverse effects
harmful if dose mixed with alcohol, headache, drowsiness, paradoxical excitement or nervousness, dizziness, vertigo, cognitive impairment and lethargy. Fall hazard for older population, have comparatively less intense effects on the normal sleep cycle, ‘hangover’ effect is sometimes reported (daytime sleepiness), withdrawal symptoms like rebound insomnia. Amnesia, anorexia, sedation, lethargy, fatigue, confusion, drowsiness, dizziness, ataxia, headache, visual changes, hypotension, weight gain or loss, nausea, weakness
Benzodiazpenes Midazolam (Versed) toxicity/management
same for all benzos
Benzodiazpenes Midazolam (Versed) interactions
same for all benzo
Benzodiazpenes Midazolam (Versed) assessment
Same for all benzos
Lorazepam (Ativan) -ANXIOLYTIC DRUGS
Mechanism of action
decrease anxiety by reducing over activity in CNS, benzos increase action of GABA (blocks nerve transmission on CNS), benzos depress activity in brainstem and limbic system
Benzodiazepenes: Lorazepam (Ativan) Indications
uses for anxiety, alcohol withdrawal, and agitation
Benzodiazepenes: Lorazepam (Ativan) Contraindications
known drug allergy, narrow-angle glaucoma, and pregnancy due to their sedative properties and risk for teratogenic effects
Benzodiazepenes: Lorazepam (Ativan) Adverse effects
CNS depression and rebound disinhibition (sedation for 1-2 hours followed by agitation and confusion), increase risk for falls in older adults. Amnesia, anorexia, sedation, lethargy, fatigue, confusion, drowsiness, dizziness, ataxia, headache, visual changes, hypotension, weight gain or loss, nausea, weakness
Benzodiazepenes: Lorazepam (Ativan) Interactions
- alcohol and CNS depressants can result in additive CNS depression and even death
- Serious consequence more likely to occur in patients with renal or hepatic compromise, oral contraceptives, azole antifungals, SSRIs
Benzodiazepenes: Lorazepam (Ativan) Assessment
assess for cautions, contraindications, and drug interactions
- prescriber may order lab studies; CBC, serum electrolyte levels, and hepatic/renal function
- assess blood pressure, alertness, orientations, sensory/motor functioning, thorough medication profile, give med cautiously under very close supervision if patient is suicidal; may be associated with suicidal attempts
Benzodiazepenes: Lorazepam (Ativan) Implementation
frequent monitoring of vitals with special attention to BP and postural BP readings, encourage use of elastic compression stocks and change positions to minimize dizziness, check for possibilities of patient holding drugs in mouth, create a therapeutic environment for discussing any disturbing thoughts such as suicidal thoughts
Benzodiazepenes: Lorazepam (Ativan) Patient teaching
encourage patients to avoid operating machinery and driving, educate development of tolerance, instruct patient not to take OTC or herbal supplements w/o taking to prescriber, advise to not use drugs that contradict, advise patients to wear medical alert or other ID with their diagnosis and list of their drugs/allergies updated every 3 months, meds need to be taken as order avoiding withdrawal
Central Nervous System Depressants and Muscle Relaxant: Kava Mechanism of action:
central nervous system depressant
Central Nervous System Depressants and Muscle Relaxant: Kava indications
common use for relief of anxiety, stress, restlessness, and promotion of sleep
Central Nervous System Depressants and Muscle Relaxant: Kava contraindications
in patients with Parkinson’s disease, liver disease, depression, or alcoholism, in those operating heavy machinery, and in pregnant and breastfeeding women
Central Nervous System Depressants and Muscle Relaxant: Kava Adverse effects
skin discoloration, possible accommodative disturbances and pupillary enlargement, scaly skin (with long term use)
Central Nervous System Depressants and Muscle Relaxant: Kava interactions
alcohol, barbiturates, psychotic drugs. May increase the effect of barbiturates and alcohol
Central Nervous System Depressants and Muscle Relaxant: Kava Patient teaching
extended continuous intake can cause a temporary yellow discoloring of the skin, hair, and nails
Herbal therapy and dietary supplement: Valerian Mechanism of action
central nervous system depressant
Herbal therapy and dietary supplement: Valerian Indication
common use for relief of anxiety, restlessness, and sleep disorder
Herbal therapy and dietary supplement: Valerian contraindications
patients with cardiac disease, liver disease, or those operating heavy machinery including treatment of insomnia, moderate sedation, muscle relaxation, anticonvulsant therapy, and anxiety relief.
Herbal therapy and dietary supplement: Valerian Adverse effects
central nervous system depression, hepatotoxicity, nausea, vomiting, anorexia, headache, restlessness, insomnia
Herbal therapy and dietary supplement: Valerian interactions
increases CNS depression if used with sedatives, monamine oxidase inhibitors, phenytoin, may have enhanced relative and adverse effects when taken with other drugs (including other herbal products) that have known sedative properties (including alcohol)
Herbal therapy and dietary supplement: St. Johns wort Indication
depression, anxiety, sleep disorders, nervousness
Herbal therapy and dietary supplement: St. Johns wort contraindications
patients with bipolar depression, schizophrenia, Alzheimer’s disease, and dementia
Herbal therapy and dietary supplement: St. Johns wort adverse effects
GI upset, allergic reactions, fatigue, dizziness, confusion, dry mouth, possible, photosensitivity (especially fair skinned)
Herbal therapy and dietary supplement: St. Johns wort interactions
may lead to serotonin syndrome if used with other serotonergic drugs (selective serotonin reuptake inhibitors). May interact with many drugs, including antidepressants, antihistamines, digoxin, immunosuppressants, theophylline, and warfarin, benzodiazepines & other hypnotic drugs. Cyclosporin and other immunosuppressants, tyramine-containing foods, opioids, digoxin, HIV drugs, oral contraceptives
Benzodiazepene (antagonist):
Flumazenil (Romazicon)
Mechanism of action: short half-life and duration effects of 1-4 hours, therefore if used to reverse the effects of a long-acting benzo, the dose of the reversal drug may wear off and the patient may become sedated again-requiring more Flumazenil.
Indications: used to acutely reverse the sedative effects of benzodiazepines. It antagonizes the action of benzo on the CNS but directly competing with the benzos for binding at the receptors. Used in cases of overdose or excessive IV sedation.
Sedative Hypnotic: Zolpidem (Ambien)
Drug Class: Non-Benzodiazepines, CNS Depressant
Mechanism of action: Depresses activity in the CNS. Specifically the hypothalamic, thalmic, and limbic system
Indications: Induces sleep & reduces agitation & anxiety related to depression and acute seizure disorders
-Women maximum dose 5mg (This is strict)
-Men maximum dose 5mg-10mg (Strict)
Contraindications: If pt allergic to aspirin, they will be allergic to this
Contraindications for ALL sedative hypnotics
Known drug allergy, narrow angle glaucoma, and pregnancy
Adverse effects for ALL sedative hypnotics
Headache, drowsiness, paradoxical excitement or nervousness, dizziness & vertigo, cognitive impairment and lethargy. May feel a “hangover” effect.
Interactions for ALL sedative hypnotics
- CNS depressants (alcohol, opioids, muscle relaxants)
- Herbal supplements: Kava & Valerian
- Nograpefruit juice or grapefruit. (alters drug metabolism-inhibition of cytochrome)
Toxicity treatment for sedative hypnotics: Zolpidem (Ambien), Restoril (temazepam)
Flumazenil
Nursing assessment for sedative hypnotics: Zolpidem (Ambien), Restoril (temazepam)
Perform assessment focusing on patient’s insomnia, with attention to onset, duration, frequency, and pharmacologic/non-pharmacologic measures. Concerns voiced by the family. Allergies, use of alcohol, smoking history & over the counter herbal supplements. Closely monitor those who are anemic, suicidal, or have history of abusing drugs, alcohol, or other substances.
Implementation for sedative hypnotics: Zolpidem (Ambien), Restoril (temazepam)
If taking medication in hospital then patient must use safety precautions, such as side rails or bed alarm. Ambulation after medication is taken (bathroom) must have assistance from nurse.
Patient teaching for sedative hypnotics: Zolpidem (Ambien), Restoril (temazepam)
Keep journal of sleep patterns. Caffeine should only be consumed in the morning, follow drug regimen, time restraints related to driving, drug interactions, hangover effects may occur, effect that grapefruit has on benzodiazepines
Muscle relaxants: Cyclobenzaprine (Flexeril) mechanism of action
Works with in the CNS. Most are known as Centrally acting skeletal muscle because of their site of action. Effects of the drug come from the sedative effects and not the direct muscle relaxation. There is no direct effect on the muscle, itself.