NUR140 Week 12 Safety

Parkinson’s, Alzheimer’s, Myasthenia Gravis, Anxiety/Depression, Sedative, Seizures

states affected by anxiolytic and hypnotic drugs

anxiety, sedation, hypnosis

benzodiazepines actions and indications

actions: act in the limbic system and the RAS; makes GABA more effective

indicated for anxiety and panic disorders, alcohol withdrawal, seizure disorders, insomnia

benzodiazepines - drugs

• alprazolam- Xanax***

• Lorazepam –Ativan***

• Temazepam-Restoril***

benzodiazepines - contraindications and cautions

glaucoma, acute alcohol intoxication (can increase CNS depression), use caution in older adults and debilitated patients (risk for falls)

benzodiazepines adverse effects

sedation, drowsiness, depression, “sleep driving”, confusion, constipation or diarrhea, nausea and vomiting

benzodiazepines drug-drug interactions

increased risk of CNS depression when taken with alcohol or other CNS depressants

decreased effects if taken with theophylline

may increase in effect when taken with cimetidine, oral contraceptives, or disulfiram

Barbiturates actions and indications

actions: depress the CNS, cerebral cortex, and motor output; causes sedation, hypnosis, anesthesia, and in extreme cases, coma

indications:relief of signs and symptoms of anxiety,insomnia, seizure disorders, and induction of anesthesia; Parenteral forms may be used for the treatment of acute manic reactions and many forms of seizures

barbiturates adverse effects

more severe

CNS depression, GI signs and symptoms, serious hypoventilation

Antihistamines - drugs to know

promethazine, diphenhydramine (benadryl)

antihistamines actions

Preoperative medications and postoperative to decrease the need for narcotics

Dexmedetomidine (Precedex)

A sedative used in medical procedures, primarily for sedation in intensive care, that provides anxiolysis and sedation without the respiratory depression typical of other sedatives.

Buspirone (generic):

An anxiolytic medication used to treat generalized anxiety disorder, producing effects without sedation or dependence.

Eszopiclone (Lunesta***)

is a prescription sleep medication that helps to improve sleep onset and maintenance, often used for insomnia.

nonbenzodiazepines - drugs

• zolpidem tartrate (Ambien)

• eszopiclone (Lunesta)

epilepsy

a chronic neurological disorder characterized by recurrent seizures due to abnormal electrical activity in the brain.

not a single disease

tonic-clonic seizures

are a type of seizure that involves loss of consciousness, body stiffening (tonic phase), and rhythmic jerking (clonic phase). They can affect both sides of the body and are one of the most common types of seizures in epilepsy.

absence seizures

are brief episodes of impaired consciousness, typically lasting a few seconds, which may involve subtle body movements or a blank stare. They are most common in children and can sometimes go unnoticed.

myoclonic seizures

are characterized by sudden, brief muscle jerks or twitches. They usually occur in clusters and may affect a specific part of the body or the whole body.

febrile seizures

are convulsions triggered by fever, often affecting young children. They typically occur during a rapid increase in body temperature and are usually harmless.

atonic seizures

are characterized by sudden loss of muscle tone, resulting in a collapse or fall. Often referred to as "drop attacks," they can lead to injuries due to falls.

status epilepticus

is a serious medical condition characterized by prolonged seizures or repeated seizures without recovery in between. It requires immediate medical intervention to prevent lasting injury or death.

focal seizures

are seizures that originate in one specific area of the brain, potentially causing changes in awareness, movement, or sensations. They may be simple or complex, depending on the level of consciousness affected.

What kind of seizure requires different drugs than other generalized seizures?

Absence seizures

Hydantoins / Anticonvulsants - drugs to know

phenytoin (Dilantin)

less sedating and less dependency forming than barbiturates or benzodiazepines

can be cost-effective

Hydantoins actions and indications

• Stabilize nerve membranes throughout CNS directly by influencing ionic channels in cell membranes, thereby decreasing excitability and hyperexcitability to stimulation

• Reduce tonic–clonic, muscular, and emotional responses to stimulation

TAPER SLOWLY

Barbiturates and Barbiturate like drugs (to treat seizures)

Phenobarbital (Solfoton, Luminal)

Primidone (Mysoline)

Barbiturates and Barbiturate-like drugs actions and indications

Used to induce sedation, manage anxiety, and control seizures by depressing the central nervous system. They enhance the effect of the neurotransmitter GABA, leading to increased inhibitory effects.

Benzodiazepines (anti-epileptics) - drugs

• Clobazam (Onfi, Sympazan)

• Clonazepam (Klonopin)

• Diazepam (Valium)

benzodiazepines (used as anti-epileptics) actions and indications

• May potentiate effects of GABA

• Cause muscle relaxation and relieve anxiety

• Stabilize nerve membranes throughout CNS

Succinimides (not in med list) - drugs

Ethosuximide (Zarontin), Methsuximide (Celontin)

succinimides actions and indications

frequently used for absence seizures

Ethosuximide should be tried first

Suppress the abnormal electrical activity in the brain that is associated with absence seizures

Drugs that modulate the inhibitory neurotransmitter GABA (anti-epileptics)

Actions and indications

• Divalproex (Depakote)***

• Valproic acid (generic)

• Valproic acid: reduces abnormal electrical activity in the brain; may increase GABA activity at inhibitory receptors

• Divalproex: action thought to be related to increased GABA levels in brain

Valproic acid and divalproex adverse effects

CNS effects, Liver toxicity, hyperammonemia, thrombocytopenia, pancreatitis

Carbamazepine actions and indications

• Treatment of generalized and focal seizures, trigeminal neuralgia; thought to inhibit polysynaptic responses and block sodium channels

Carbamazepine adverse effects

CNS effects; blood dyscrasias; edema, HTN, and fluid overload; dermatitis, rash, photosensitivity, Stevens–Johnson syndrome

Carbamazepine drug-drug interactions

CNS depressants, CYP3A4 inhibitors and inducers, concomitant drugs, topiramate

levetiracetam (Keppra) actions and indications

Mechanism of action not completely understood; may be related to suppression of rapid action potentials

indicated for seizures

Levetiracetem adverse effects

CNS effects, including drowsiness and fatigue; psychiatric symptoms; dizziness; and potential for renal impairment.

• Topiramate (Topamax) *** actions and indications

Topiramate is an antiepileptic drug that works by reducing the frequency of seizures and is indicated for both epilepsy and migraine prophylaxis.

Topiramate adverse effects

Marked CNS depression, metabolic acidosis, angle closure glaucoma, suicidal thoughts and behavior, etc.

Topiramate drug-drug interactions

Phenytoin or carbamazepine, oral contraceptives

Pregabalin (Lyrica) *** and Gabapentin (Neurotin) ***

actions and indications

• Stabilize nerve membranes in different ways

  • Alter sodium or calcium channels

  • Increase the activity of GABA

Antiepileptic

Parkinson’s Disease

A progressive neurodegenerative disorder affecting movement control, characterized by tremors, rigidity, and bradykinesia.

Causes unknown

No cure

Therapy aimed at management

May develop in people at any age

symptoms of parkinson’s

tremors, bradykinesia, rigidity, postural instability, and impaired balance.

Dopaminergics (for parkinson’s) - drugs to know

Carbidopa-Levodopa, Pramipexole, Ropinirole

Dopaminergics actions and indications

• Promote dopamine synthesis, activate dopamine receptors, prevent dopamine breakdown, or decrease degradation of levodopa

• Help to restore balance between inhibitory and stimulating neurotransmitters

• indicated for parkinson’s

anticholinergic agents - drugs to know

Benztropine (Cogentin)*

anticholinergic agents actions and indications

• Therapeutic actions

  • Have greater affinity for receptor sites in CNS than for those in peripheral nervous system

• Indications

  • Treatment of parkinsonism

  • Relief of symptoms of extrapyramidal disorders associated with use of some drugs

anticholinergic drugs adverse effects

may include dry mouth, blurred vision, constipation, urinary retention, and confusion.

Dopamine Agonists - drugs to know

pramipexole (Mirapex) and ropinirole (Requip)

dopamine agonists actions and indications

• Pramipexole (Mirapex) *** treatment of idiopathic (cause unknown) Parkinson’s disease

• Ropinirole HCL (Requip) *** treatment of idiopathic Parkinson’s disease in early stages and in later stages

  • when combined with levodopa: treatment of restless leg syndrome also.

drugs used to improve patient response to initial therapy in parkinson’s disease

(adjunctive therapy)

• Entacapone (Comtan)

• Safinamide (Xadago)

• Selegiline (Eldepryl)

• Tolcapone (Tasmar)

Acetylcholinesterase Inhibitors - drugs to know

• Pyridostigmine bromide (Mestinon)***

• Tacrine HCL (Cognex)*** Cognex (tacrine hydrochloride) is a reversible cholinesterase inhibitor used to treat patients with Alzheimer's disease or mild to moderate dementia. Cognex is discontinued in the U.S., but generic versions may be available.

• Donepezil (Aricept)***

• Memantine (Namenda)*** Box 32.7 p 560

Acetylcholinesterase Inhibitors actions and indications

These drugs inhibit the enzyme acetylcholinesterase, increasing acetylcholine levels in the brain, and are primarily indicated for the treatment of Alzheimer's disease and certain dementias.

• Indications

  • Myasthenia gravis

  • Alzheimer’s disease

  • Glaucoma

  • Treatment after exposure to nerve gas

myasthenia gravis

a chronic autoimmune condition that affects the communication between nerves and muscles, leading to weakness in skeletal muscles.

patients make antibodies to nicotinic AcH receptors

symptoms of Alzheimer’s disease

include memory loss, confusion, difficulty in completing familiar tasks, difficulty in language, apathy, changes in mood or behavior, and impaired judgment.

no cure