Pharmacology: Stimulants and Anticonvulsants Debbie Amason, RN, BSN, MS CNS- Stimulants Chapter 19 *These meds are medically

y approved for: Attention deficit hyperactive disorder ( ADHD) caused by a disregulation of transmitter serotonin, norepinepherine, and dopamine. Common in children. More common in boys. Narcolepsy characterized by falling asleep during normal waking activities Obesity Respiratory depression Major Groups *Amphetamines stimulate the release of norepinepherine and dopamine from the brain *Analeptics stimulate respirations *Anorexiants treat obesity Pathophysiology *ADHD- disregulation of transmitters serotonin, norepinephrine, and dopamine Usually children prior to age 7, more common in boys See poor coordination, possible abnormal EEG *Narcolepsy- falling asleep during normal waking hours. Usually accompanied by sleep paralysis ( the condition of muscle paralysis that is normal during sleep cycle) Amphetamines *How they work? *Side effects *Uses Amphetamine-like drugs *Primary drugs used for ADHD and narcolepsy *Used to increase attention span and cognitive performance and decrease impulsiveness and hyperactivity. Ritalin- most common for ADHD Focalin Cylert- not a first line drug can cause hepatic failure *Provigil- used for narcolepsy (Ritalin and cylert also used for narcolepsy) Increases time patient feels awake *Pharmacokinetics- well absorbed from GI tract should not be given within 6 hours before sleep should be given before meals *Pharmacodynamics decongestants enhance actions of Ritalin and cylert *Nursing process Stimulate release of neurotransmitters norepinephrine and dopamine from brain and peripheral nervous system Short term Long term

Assessment If there is hx of heart diease, hypertension, hyperthyroidism, parkinsonism, or glaucoma, usually contraindicated. Pay close attention to PT with cardiac conditions. *Teaching - before meals avoid alcohol encourage sugarless gum to relieve drymouth report all weight loss to physician avoid hazardous activities when feeling tremors or nervousness fo noy sntuply fidvonyinur ftuh avoid caffine (even in OTC pills) not good for nursing mothers encourage family conseling explain long-term use/drug abuse connections

Anorexiants *Amphetamine appetite suppressants Use short term to treat obesity Disadvantages tolerance, psychological dependence, and abuse FDA restrictions ordered removal of phenylproanolamine from OTC weight loss remedies and cold drugs b/c hemorrhage risks for women. Side effects nervousness, restlessness, irritability, insomnia, heart palpitations, and hypertension Drugs Didrex Dexedrine Dospan, Tenuate, Tepanil Fastin, Ionami, Zantryl (w/out phenylpropanolamine) Acutrim, control, dexatrim, texatrim Natural, Prolamine

Analeptics *Mostly affect brain stem and spinal cord but also cerebral cortex. Primary use- stimulate respirations *Xanthines Caffeine stimeulates CNS large doses stimulate Respiration

(sometimes given to newborns in repiratory distress Theophylline relaxes bronchioles Side effects *Nervousness, restlessness, tremors, twitchings, palpitations, *Insomnia, diuresis, GI irritation, tinnitis, dependence Respiratory CNS Stimulant *Doxapram (Dopram) *Used to treat respiratory depression caused by drug overdose, pre and post op anesthesia, COPD *Given IV *Onset 20-40 seconds *Peak- 2 minutes *Side effects - hypertension, tachycardia, trembling, convulstions Headaches: Migraines *Characterized by unilateral throbbing head pain accompanied by nausea, vomiting, and photophobia *Symptoms persist 4-24 hours, and for some lasts several days. 2/3 occur in women Ages 20-30 Symptoms decrease with pregnancy and menopause *Pathophysiology caused by inflammation and dilation of the blood vessels in the cranium; suggested imbalance in neurotransmitter [5-HT] ; cheese, chocolate, and red wine can trigger an attack *2 types - Classic migraines associated with an aura that occurs minutes to 1 hour before onset Common migraines not associated with an aura

Headaches: Clusters- characterized by unilateral throbbing usually around eye. Series of attacks every day for several weeks no aura no nausea and vomiting Treatment of Migraine Headaches Treatment depends on intensity of pain *Beta-adrenergic blockers- Inderal, Atenolol *Anticonvulsants- Depakote, neurontin *Tricyclic antidepressants- Elavil, Tofranil *Drugs chosen depend on severity and include analgesics, opioid analgesics, ergot alkaloids, selective serotonin receptor agonists (triptans)

Anticonvulsants Chapter 22

*Epilepsy- seizure disorder Occurs 1% population Occurs r/t abnormal electrical discharges from the cerebral neurons and is characterized by loss or disturbance of consciousness and convulsion. *Diagnosis EEG - electroencephalogram CT computerized tomography MRI magnetic resonance imaging Classification of Seizures *3 types Grand-mal tonic-clonic most common form Tonic sustained muscle contraction - skeletal muscles contract in a spasm, lasting 3-5 seconds Clonic dysrhythmic muscle contraction or jerkiness lasting 2-4 minutes Petit-mal absence seizure brief loss of consciousness lasting less than 10 seconds- usually occurs in children less than 3 spikes on EEG Psychomotor *2 categories General convulsive and non convulsive; involve both hemispheres of the brain Partial Involve one hemisphere of the brain. No loss of consciousness in simple partial seizures, but there is a loss of consciousness in complex partial seizures

Anticonvulsants/antiepileptic suppress abnormal electric impulse from seizure focus to other cortical area, thus preventing the seizure but not eliminating the cause of the seizure. *Drugs types Hydantoins Barbiturates Benzodiazepines Carbamazepines Valproate Succinimides *Each drug not appropriate for every type of seizure Anticonvulsants *How they work? Suppress abnormal electrical impulses from seizure focus to other cortical areas which prevent, not eliminate the cause of the seizure. 75% seizure free if medications taken Life long therapy

 History *1857- Potassium bromide *1918- phenobarbital *1938- Dilantin Pharmacophysiology *All of the medications work in 1 of 3 ways Suppress Na+ influx thru drug binding to the Na channel when inactivated leads to prolonged inactivation, prevents firing of neurons Suppress Ca influx to prevent electrical current generated by Ca ions to T calcium channel Increase action of gamma aminobutyric acid (GABA) which inhibits neurotransmitter throughout brain Hydantoins *Most common used today *Least toxic effects *Small effect on general sedation *Non addicting *Teratogenic SHOULD NOT BE USED WITH PREGNANCY *Pharmacokinetics absorbed in Small intestine - HIGHLY protein bound half like is 22 hours *Pharmacodynamics PO action @ 30 minutes to 2 hours. Peak serum @ 1.5-3 hours. IV should be direct injection, no mixing with dextrose. CONTINUOUS IV should not be used. Do NOT do IM. *Side effects gingival hyperplasia Short term slurred speech, confusion, depression, low platelet/WBC count Long term elevated blood sugar *Drug to drug interactions highly protein bound, compete with anticoagulants and aspirin for binding sites. Cimetidine (tagamet) can increase action of hydantoins by inhibiting liver metabolism. Herbal interactions primrose and borage may lower seizure threshold, that may need modification. Ginkgo may decrease pheytoin effectiveness. Barbiturates *Long acting medication used to treat grand mal seizures and status epilepticus seizures. *Fewer teratogenic effects on fetus than Dilantin *Disadvantages Addictive/ tolerance build up Causes General sedation Must discontinue gradually to avoid recurrence of seizures Succinimides *Primary use is for petit mal/absent seizures *May used in conjunction with other meds *Drug of choice

zarontin

Oxazolidones *Primary use is for treating petit mal seizures *Not used as often because of side effects *Drug- Tridione Benzodiazepines *3 drugs used as anticonvulsants *Klonopin- petit mal *Tranxene- partial seizures *Valium- Acute status epilepticus has a short term effect *Status Epilepticus =medical emergency *Rapid succession of seizures or continuous seizure state Iminostilbenes *Tegretol- used to treat refractory seizure disorder that have not responded to other therapy *Used for grand mal and petit mal seizures *Medication used for other disorders Bipolar disorder Trigeminal neuralgia ETOH withdrawal Miscellaneous *Drugs of choice today are: Neurontin Lamictil Topamax Anticonvulsants and Pregnancy *Seizures increase 25% in pregnancy *Danger is hypoxia places woman and fetus at risk *Drugs increase loss of folic acid which increases risk for neural tube defects *Inhibit Vitamin K *Many drugs are teratogenic Febrile Seizures *Seizure associated with fever occur in children between 3 months and 5 years *2.5% children develop epilepsy if have 1 or more febrile seizures Calproic acid should not be given to children b/c of its possible hapotoxic effects.