Test 2

Drug Definition
Parikinson's Disease neurodegenerative disorder of the extrapyramidal system associated with disruption of neurotransmissions (DA, ACH) within the striatum, Dyskinesias, Akinesia, Degeneration of neurons that make DA
Dyskinesias tremors at rest, rigidity, postural instability, bradykinesia
Levodopa DA replacement, converts to DA in brain then activates receptors(used with carbidopa to block degradation of levodaopa in periphery, first line drug or supplement to DA agonist, requires drug holiday or effects will diminish
Bromocriptine DA Agonist, direct activation, first line or supplement to levodopa
Pramipexole (mirapex) D2 receotir agonist, Nausea, nonergot agents, prefered, Same as Ropinrole; bromocriptine & pergolide
Entacapone(Comtan) COMT Inhibitors, stops breakdown of levodopa, adjunct to levodapa to increase "on time" and decreased "wearing off" preferred over tolcapone(liver failure, dyskinesias, nausea)
Amantadine(symmetrel) DA releaser; Antiviral; promotes DA release from reaming neurons;may also block re uptake; second line for motor fluctuations
Selegiline(Edepryl, Carbex) MAO-B Inhibitor; stops brealdown of DA by MAO-B; used in newl diagnosed patients for possible neroprotection, second or third line as adjunct to levodopa; varirous drug interactions (prozac)
Dopaminergic Agents Mechanism of action Promotion of Dopamine synthesis; prevention of DA degradation; promotion of DA release; Direct activation of receptors
Decarboxylase Pyridoxine changes Levodopa to Dopamine, vitamine B6 increases its reactivity
Anticholinergic Agents Used since 1867, used today as second-line for tremor; mech of action: blockade of muscarinic cholinergic receptors in striatum, block in periphery; cause dry mouth, blurred vision, photophobia, urinary retention, constipation & tachycardia; glaucoma aggr
Trihexyphenidyl(artane) Anticholinergic Agent for younger patients with mild symptoms
Benzotropine(congentin) Anticholinergic Agent for younger patients with mild symptoms
Alzheimer's Disease key areas of brain are destroyed; steady delcine in mental function, Neurofibrillary tangles; senile plaques, degen of neruons, reduced cholnergic Transmission, B-amyloid and neutric PLaques, apoE4, ER assiociated binding protien, homocysteine
Risk Factors of Alz Major: advancing age, family history; Possible: female, head injury, low educational level, production of apoE4, high levels of Homosysteine, Nicotine in cigarret smoke
symptoms of Alz Memory Loss, confusion & Disorientation, impaired judgment, personality changes, difficulty with self-care, behavior problems, inability to recongnize family memebers, inability to communicate
Cholinesterase Inhibitors drug therapy for Alz patients, for mild to Moderate, slows progression; side affects, cholinergic side effects, GI, Dizziness, headache, Bronchoconstriction, liver injury(tacine)
Tacrine(cognex) AD Cholinesterase Inhibitor 1993, rarely used due to hepatoxicity & dosing
Donepezil(Aricept) AD Cholinesterase inhibitors
1996 drug of choice 1/day
Rivastigmine(Exelon) AD 2000, Cholinesterase inhibitors
"irreversible", no significant drug interactions
NSAIDs-AD 2 year therapeutic gap(52)
Vitamein E & Selegiline (antioxidents) a vitamen and MAO-B inhibitor, do not affect core characteristics of AD, not synnergystic, only slow progression
MS a chronic, inflamatory autoimmune disorder that damages the melin sheath of neurons in the CNS, vaietu of sensory and motor deficits, relaspse and remissions, progressive
MS-S&S vary depending on where CNS demylination accurs and the size of the region, paresthesias, motor problems, visual impairment, bladder and bowl, sexual dysdunction, fatigue, emotional lability, depression
Subtypes of MS Relapsing Remitting, Secondary progressive(R&R then progressive), Primary progressive, Progressive Relapsing
Immuno-modulators 4 availble, rec. for all patients with R&R MSand secondary prog. w/ accute exaerbations, decrease relapse rate by 30%; self injected
Interferon Beta (MS) naturally occurring glycoprotien with antiviral, antiproliferative and immnuomodulatory actions,; reduces the frequency and severity of attacks; reducaes the number and size of MRI detectable lesions; delays progression of disbility;
Interferon Beta (MS) Adv. Effects flu-like, hepatoxicity; myelsuppression; Injection-site reactions; depression; drug interactions;
Glatiramer Acetate(Copaxone) Long term therapy of R&R MS; protects myelin by inhibiting immune response to meylin basic protien; well tolerated
Immuno-suppressants only 1 approved by FDA Mitoxatrone (Novantrone); more toxic than immuno-modulators; targets B&T lymphocytes and Macrophages; produces greater suppresion of immune function-comparable to chemo
Mitoxantrone(Novantrone) dec. neurologic disability and clinical relapse; binds with DNA and inhbits Topoisomerase; myelosuppresion cardiotoxicity fetal harm;
Monitoring summarry of Mitoxantrone Complete blood counts at baseline and prior to each dose; liver function test "", pregnancy test ""; determine LVEF: prior to first dose, prior to all doses once the cumulative dose has been reached, whenever signs of CHF develop
Epilepsy group of disorders charaterized by excessive neuron stim. within the CNS; seizure – partial (focal) seizures or generalized seizures; MOA of drug Therapy- suppresion excitation; enhance inhibition
Partial (focal) Seizures Simple – no loss of conciousness 20-60sec; Complex Partial – impaired conciousness, fixed glare, followed by repetitive pointless movement 45-90sec; secondary generalized – begin as simple or complex and evolve into tonic-clonic, no concious, 1-2min
Generalized Seizures Tonic-clonic(grand mal) – rigidity to synchronous muscle jerks followed by cns depression (prostictal state) 90sec or less; Absence(petit mal) – loss of conc. 10-30 sec,mild symettric activity; Myoclonic – sudden muscle contractions 1 sec; atonic – drop
Status Epilepticus 30 minutes many types
Epilepsy: therapeutic Considerations Treatment: Neurosurgery(best sucess rate), Vagal NErve Stimulation, Ketogenic diet; Diagnosis and drug selection, drug evaluation, monitoring plasma drug levels, promoting patient adherence, withdrawing antiepileptic drugs
Anti-epileptic Drugs (AED) Suppress discharge or neurons with seizure focus, supress propagation of seizure activity from the focus to other areas of the brain; supress NA, CA influx, and potentiation of GABA
Phenytoin(Dilantin) Partial and tonic-clonis; selective inhibtion of NA channels; varied oral absorption, half-life 8-60 hours; used following Valium after a SE seizure; old class; adv: nystagmus, gingival hyperplasia, skin rash, sedation, ataxia, diplopia, cog im
Drug interactions of Phenytoin dec effect of oral contraceptives, warfarin, glucocorticoids; diazepam, isoniazid, cimetidine, alcohol, valproic acid increase levels, Fosphenytoin, better for IV delivery, a pro-drug of phenytoin
Carbamazepine(tegretol) old class, partial & tonic-clonic seizures, not absence, bipolar disorders, trigeminal and glossopharyngeal neuraglias; MOA, delayed recovery of NA channels;
adv effevts of Carbamezepine Neurologic effects (nystagmus, ataxia), Hematologic effects (leukopenia, anemia, thrombocytopenia), birth Defects, hypo-osmolarity(H20 retention); rash, photosensitivty reactions
Ethiosuximide(Zarontin) drug of choice for abscence seizures, only for absence; suppresses T-currents in thalamix neurons
Phenobarbital one of oldest, enhance gaba response, barb, low doses cns depressent, effective inexpensive & once a day, partial and tonic-clonic, promotes sleep and sedation, side effects – depression & learning impairment, dependance
Valporic Acid(Depakene, Depakote, Depacon
old class seizure, bipolar, migrain; MOA=NA Ca channels and GABA; Adv. GI effects, hepatoxicity, pancreatitis, teratogenic
Oxcarbazepine(trileptal) newer AED carbazepine-derived,better tolerated, but expensive
Lamotrigine[Lamictal] newer AED limited use, not for under 16, life threating rashes.
Gabapentin[Neurontin] newer AED limited use, enhances GABA release, well tolerated.
Levetiracetam[Keppra] adjunctive for partial seizures in adults, unknown MOA, well tolerated.
Topiramate[Topamax] newer AED adjunctive, multiple MOAs, glaucoma.
Tiagabine[Gabitril] newer AED adjunctive, GABA reuptake blocker, well tolerated.
Zonisamide[Zonegran] newer AED adjunctive, sulfonamide antibiotic, multiple MOA (Na+ & Ca++ channels), many AEs.
Vigabatrin[Sabril] newer AED inhibits GABA breakdown, not available in the USA.
Felbamate[Felbatol] newer AED unknown MOA, potentially fatal AEs.
Muscle Spasm involuntary contraction of muscle or muscle group; epilepsy, hypocalcemia, pain syndromes, trauma,
Muscle spasticity cns derived movement disorders: MS CP, traumatic spinal cord lesions or stroke, heightened muscle tone spasm loss of dexterity
Baclofen(Lioresal) GABA agonist, Acts in the spinal cord, Suppresses hyperactive reflexes, Decreases flexor and extensor spasms, Suppresses resistance to passive movement , No direct effect on skeletal muscle
Diazepam(Valium) Acts in the central nervous system; GABA modulator; muscle relaxant; no antidote, gradual with draw 1-2wk, CNS dep, nausea constipation, urinary retenion
Dantrolene(Dantrium) Acts directly on muscle, Suppresses the release of calcium from the sarcoplasmic reticulum (SR); Spasticity associated with multiple sclerosis, cerebral palsy, spinal cord injury, Malignant hyperthermia; hepatoxicity, muscle weakness, drowsines
Tizanidine(Zanaflex) Through agonist action of alpha2 receptor
Local Anesthetics Stop axonal conduction by blocking sodium channels, Block all neuronal function, both sensory and motor; use with vasoconstrictors (epi), blood esterases and liver enzymes eat em, CNS excitation followed by dep., depress cardiac excitability, vasodil,alle
Procaine(Novocain) used with epi, allergic reactions to ester-type
Lidocaine amide type, widely used control dysrhythmias;
cream, ointment, jelly, solution, aerosol, patch
cocaine ester-type, used in ear, nose & throat procedures, CNS excitation, depression, CV- sympathetic stim, & NE uptake block (hypertension, dysrhythmias, angina)do not need epi, topical only, produces euphoria, physical dependance, avoid w/ cardiac patients
General Anesthetics Produce Unconsciousness Lack of response to all painful stimuli; 2 groups Inhalation and IV
Inhalation Anesthetics purpose Unconsciousness, Analgesia, Muscle relaxation, Amnesia, Induction brief and pleasant, easy to titrate, high margin or safety, emergence brief and pleasant.
Balanced Anesthesia Combinations of drugs consisting of:Short-acting barbiturates (induction), Neuromuscular blocking agents, Opioids (analgesia), Nitrous oxide (analgesia)
Preanesthetic Medications Benzodiazepines, Barbiturates (pentobarbital), Opioids, Clonidine, Anticholinergic drugs (? bradycardia), Neuromuscular blocking agents, anxiety, perioperatice amnesia, post and preoperative pain
Post-anesthetic Medications Analgesics, Antiemetics[Ondansetron (Zofran)], Muscarinic agonists [Bethanechol] Bowel atony, urinary retention,
Inhalation Anesthetics Halothane, Isoflurane (most widely used), Enflurane, Desflurane, Sevoflurane, Nitrous oxide
Halothane Analgesia, Muscle relaxation; adv. hypotension, respiratory depression, promotion of dyrhythmias, malignant hyperthermia, hepatoxicity
Thiobarbiturates (short-acting), IV, induction of anesthesia, Thiopental (Pentothal)
Benzodiazepines Diazepam (Valium) & Midazolam (Versed)
Propofol(Diprivan) Respiratory depression & hypotension, Bacterial infection
Etomidate (amidate) potent hypnotic, no analgeisa, preferred to barbiturates if CV concerns exist, hypotension, oliguria, elctrocyte disturbances, & postoperative nausea and vommiting
Ketamine(ketlar) Dissociative anesthesia, avoid if history of psychiartric illness exists
Droperidol plus fentanyl(innovar) antipsychotic + opiod, neurolept analgesia, appears asleep, QT interval prolongation with droperidol
Neuromodulation of Pain Bradykinin, histamine, prostagladins, substance P, neurokinin A and peptides cause spread of localized pain, endorphins inhibit
Morphine prototype of strong opiods from seedpod of poppy, pain relief drowsiness, mental clouding, anxiety reduction, sense of well-being, decrease sensation of & emotional reaction to pain
Morphine Adv effects respiratory depression(tolerance), constipation (little tolerance). Orthostatic hypotension (blunts baraoreceptors) urinary reteintion (monitor output) biliary colic, cough suppression, emesis(stims the CTZ), increased ICP(dec respiration, inc co2, vasod
Pharmacokinetics of morphine admin by oral, IM, IV, subcutaneous, epidural and intrathecal
Morphine drug interactions CNS depressants (Ethanol), Anticholinergic drugs, Hypotensive drugs, Monoamine oxidase inhibitors, Agonist-antagonist opioids, Opioid antagonists
other strong opioid agonists Fetanyl: parenteral(sublimaze), transdermal (duragesic), transmucosal (actiq), methadone, heroin
Agonist-Antagonist Opioids Pentazocine(Talwin)Analgesia, limited euphoria & ? respiratory effects; Nalbuphine (Nubain); Butorphanol (Stadol); Buprenorphine (Buprenex – IM or IV, Subutex – sublingual)
Naloxone opioid overdose, postoperative opoid effects, neonatal respiratory depression
Opioid Overdose Classic triad Coma, Respiratory depression, Pinpoint pupils, treatment: Ventilatory support,Opioid antagonist
Cluster Headaches occur in series, attack free interval of months to years seperate clusters, prohpylaxis – prednisone, LI & verapamil
Tension-Type HEadache most common, moderate, non throbbing, pain, usually located in a head band distr., maybe episodic or chronis, treatment: nonopiod analgesic, patients learn to deal with stress
migraine facts 26 million americans have migraines, 70% women, cause 157 million missed work days, 2.8 on others, medical expense is $50 bilion/y
Migraine Symptons Nausea, vomiting, photophobia,phonophobia, hand and feet may feel cold and sweaty, interable to odors, tinnitus, blurred vision, aura
Calcitonin gene-related peptide (plasma levels rise during migraine) causes migraines by stimulating the trigeminal pathway, vasodilation
Serotonin (5HT 1b/1d) receptors activation can abort attack ( 5ht levels drop by 50% during attack) depletion of 5ht can cause a migraine
Ergotamine [Ergot Alkaloids] (exact mech unknown(5ht , DA and alpha receptors affected, well tolerated some emesis, take sublingual, oral and rectal
Dihydroergotamine [Ergot Alkaloids] drug of choice for aborting migraine and cluster headaches, nasal spray or injection
Sumatriptan (Imitrex) Serotonin1B/1D-Receptor Agonists, Oral, nasal spray, subq; adv. chest symptoms, coronary vasospasm teratogenesis
Preferred drugs for migraine prevention Beta blockers
Tricyclic antidepressants (amitriptyline) used for migraines
Antiepileptic drugs used for migraines Divalproex (Depakote) Topiramate (Topamax)
Schizophrenia Chronic psychotic illness, Characterized by disordered thinking, Reduced ability to comprehend reality, Usually emerges in adolescence or early adulthood
Conventional Antipsychotic Agents Low potency—Chlorpromazine (Thorazine), Medium potency—Loxapine, High potency—Haloperidol (Haldol)Mech: Block receptors of dopamine, acetylcholine, histamine, norepinephrine
Conventional Antipsychotic Agents adverse effects Acute dystonia (spasms – respiration), Parkinsonism, Akathisia (extreme restlessness), Tardive dyskinesia (“fly-catching”), Neuroleptic malignant syndrome, Anticholinergic effects, Orthostatic hypotension, sedation, neuroendocrine effects, seizures,
Conventional Antipsychotic Agents interactions Anticholinergic drugs, CNS depressants, Levodopa and direct dopamine-receptor agonists, Conventional antipsychotic drugs are very safe, Death by overdose is extremely rare.
Clozapine Atypical Antipsychotic Agent, prototype; Blocks dopamine and serotonin, Fewer EPS symptoms; Adverse effects: Agranulocytosis, seizures, diabetes, wgt gain, myocarditis, orthostatic hypotension, antichilonergic effect, levodopa-induced psychosis
Evidence for the monoamine hypothessi of depression Drugs that depelete MA r depressants; most antdepressants enhance monoaminergic trans. at some point in the synaptic signaling; the conc. of MA and their metabolites is reucded in the CSF of depressed; postmortem elevated 5ht binding
Clinical features of Depression depressed mood; loss od pleasures or interest; insomnia, hypersomnia; anorexia or hyper; mental slowing and loss of conc; feelings of guild; worthlessness-helpless; thoughts of death; present most of the day, for 2 weeks
Depression Treatment Modalities TCA; SSRI, MAOI, atypical antidepressants; ECT, Vagus nerve stimulation, psychotherapy
Imipramine (tofranil) TCA; 1st choice for major depression, blocks reuptake of NE and 5ht, 1/2 life long and variable; resp. 1-3 wks, maximal resp. 1-2 months
TCA Toxicity and therapeutic uses Has lethal dose; only dispense 1-week supply; antidote: cholinesterase inhibitor (physostigmine); treatment of dysrhythmias; gastric lavage followed by activated charcoal. Treats Depression, Bipolar, Neuropathic pain, chronic insomnia, AD/HD, panic, ocd
TCA adverse effects orthostatic hypotension; antichonergic effects, diaphoresis, sedation, cardiac toxicity (dysrhythmias, tachycardia); seizures, hypomania, yawngasm
TCA drug interactions MAOI, direct acting sympathomimetic drugs, indirect acting sympathomimetic drugs, anticholinergic agents, CNS depressants
SSRI uses effective as TCA, Major depression, OCD, Bulimia nervosa, panic disorders
Fluoxetine (prozac) SSRI highly protein bound, 1/2 life 2 days; steady state; adverse effects; sexual dysfunction, nausea, headache, serotonin syndrome, withdrawal, wgt gain
TCA drug interactions MAOI, Warfarin, TCA, LI
MAOI 2nd or third choice; cause irreversible inhibition in MAO-A within synaptic terminal, Depression, Bulimia, OCD, red. of panic attacks
MAOI adverse effects CNS stim, othostatic hypotension, hypertensice crisis, multiple drug-drug and drug-food interactions
MAOI dietary restrictions avoid tyramine-rich foods, yeast extracts, most cheeses aged fish or meat, figs, bannanas, wine; tyramine activates the secretion of NE in the arterioles of the heart
Bupropion(wellbutrin) atypical anti; acts as stimulant and suppresses appetite; antidepressant effects 1-3 wks; does not affect 5ht, cholin, or histamine transmisions (MOA unclear); no wgt gain; similiar struct. to amphetamines, increase sexual desire and pleasure
Advers effects of Bupropion agitation, headache, constipation, dry mouth
Bipolar Disorder cyclic disorder; recurrent fluctuations in mood, mania and depression,
Drug therapy for Bipolar Mood stabilizers: relieve symptoms during mania or dep. episodes; prevent reoccurences;do not worsen mania or depression, or accelerate the rate of cycling. Antipsychotics; given during manic episodes. Antidepressants: given during depressive episode
Galanamine(reminyl) 2001 AD cholinesterase inhibitor GI complaints
Memantine(namenda) First drug in a new class, the NMDA receptor antagonists; for moderate to sever AD, better tolerated than cholinesterase inhibitors, adv. dizziness headache confusion, constipation
Lithium simple inorganic ion, drug of choice for mania, found in animal tissues. Bipolar mood stabilization, alcoholism, bulimia, schizophrenia, glucocorticoid-induced psychosis
Lithium Pharmacokinetics abs, dist; excretion: short half-life, excreted by kidneys, in tandem with NA levels, plasma levels .8-1.4 mEg/l
Lithium Toxicity Li levels greater than 1.5 mEq/L; adv. GI, tremors, polyuria, renal toxicity, goiter and hypothyroidism, teratogenesis
AED for Bipolar Valproic acid(depakote); carbamazepine (Tegretol) reduces symptoms, protects against recurrence of mania and depression, target trough plasma level 4-12 mcg/mL; Lamotrigine(Lamictal) long term maint. alone or combo
Antipsychotic Drugs manic episodes; use for long-term to help stabilize mood; benefit patients with or without psychotic symptoms; can be combined with mood stabilizer
Benzodiazepines Drug of choice to treat inomnia and anxiety; induce generel anestheisa, manage seizure disorders, muscle spasm, panic disorder, and withdrawl from alcohol; diazepam(valium); safer than general cns depressent; lower poten. abuse; fewer drug interactions
Benzodiazepines Therapeutic Uses Anxiety, insomnia, seizure disorders, muscle spasm, alcohol withdrawl, panic disorder, perioperative applications
Benzodiazepines adverse effects CNS depression, anterograde amnesia; paradoxical effects; respiratory depression; abuse; use in pregnacy and lactation
Benzodiazepines Drug interactions and dependance CNS Depressants; Tolerance with prolonged use to some extent; dependace but incidine of substantial is low
Benzpdoazapeines Acute toxicity and prep, dosage, and admin oral overose; iv toxicity; general treatment measures; treatment with flumazenil(romazicon); taken orally and parenterally (IM and IV)
Zolpidem[Ambien] Benzodiazepine-Like Drugs; Short-term management of insomnia
Zaleplon[Sonata] Benzodiazepine-Like Drugs; New class of hypnotics, pyrazolopyrimidines; Short-term management of insomnia; Prolonged use does not appear to cause tolerance
Eszopiclone[Lunesta] Benzodiazepine-Like Drugs; Is the S-isomer of zopiclone; For treating insomnia; No limitation on how long it can be used
Barbiturates Pharmacokinetics Lipid solubility has a significant impact; Rapid onset and brief duration
Barbiturates Therapeutic uses Seizure disorders; Induction of anesthesia; Insomnia;
Barbiturates Ultrashort acting (thiopental); Short to intermediate acting (secobarbital); Long acting (phenobarbital); MOA: binds to GABA receptor-chloride channel complex
Barbiturates Pharmacologic effects CNS depression; Cardiovascular effects; Induction of hepatic drug-metabolizing enzymes
Barbiturates Tolerance and physical dependence Develops to many—but not all—CNS effects; Develops to many—but not all—CNS effects; physical depedance
Barbiturates Adverse effects Respiratory depression; Suicide; Abuse; Use in pregnancy; Exacerbation of intermittent porphyria; Hangover; Paradoxical excitement
Sleep Physiology Sleep Phases REM, NREM; I = relatively light sleep; II = relatively light sleep; III = deep sleep; IV = deep sleep
Basic Management Principles for insomnia Cause-specific therapy: Treatment is highly dependant on the cause; Nondrug therapy; Therapy with hypnotic drugs: Benzodiazepine and like drugs; trazodone (desryel) – atypical antidepressant; antihistamines; rozerem (ramelteon)
Generalized Anxiety Disorder Uncontrollable worrying that lasts 6 months or longer; Treatment: nondrug: supportive therapy, cognitive behavioral therapy, biofeedback; relaxtion training
Generalized Anxiety Disorder Drug Therapy Benzodiazepines(1st line): Alprazolam (Xanax), Lorazepam (Ativan); SSRI: Paroxetine (paxil) short and long term, escitalopram (lexapro); Atypical antidepressant: venlafaxine (effexor XR); 5-HT agonist (< DA): Buspirone (BuSpar)
Buspirone(BuSpar) 5ht agonist; Non-CNS depressant; no sedation, no abuse potential, no intensify the effects of CNS depressants, Anxiolytic effects develop slowly, well absorbed orally, taken w/ food, adv: dizzy, nausea, nervousness, light-headed, excite
Buspirone interactions (BuSpar) Grapefruit juice, erythromycin & ketoconazole
Panic Disorder Palpitations, pounding heart, racing heartbeat; Chest pain or discomfort; Sensation of shortness of breath; feel choke; dizzy lighthead, nasuea tummy ache; fear of losing cnotrol, dying, tingling numb hands, flushes or chills
Panic Disorder treatment Drugs; cognitive behavioral therapy, antidepressants: SSRI, Benzodazepines (fast relief) 1st line drug
Obsessive-Compulsive Disorder Potentially disabling condition, Persistent obsessions and compulsions; SSRI 1st line: Fluoxetine (Prozac), Fluvoxamine (Luvox), Paroxetine (Paxil), Sertraline (Zoloft;, Clomipramine (Anafranil) less tolerated second line
Social Anxiety Disorder Intense, irrational fear – might be scrutinized by others(generalize or non, public speaking) debilatating common; treatement: psychotherapy/drug; SSRI: paroxetine, sertraline; atypical: Venlafaxine (effexor XR), BZDs, BEta blockers: propanolol (inderal)
Amphetamines Release NE, DA, effect CNS amd CVS, Tolerance, dependance and abuse; treats ADHD Narcolepsy, Obesity,
Amphetamines Adverse effects CNS stim, wght loss, CVD effects Psychosis, Acute toxicity: dysrhythmias, hypertension, dizzy, confused, halluc., convulsions, paranoid delusions, coma, palpit, cerbral hemor, treat w/ chlorpromazine (anti-psychotic), alpha blok(phentolamine), Diazepam
Amphetamines Preparations, dosage, and administration Dextroamphetamine sulfate: Short duration [Dexedrine, Dextrostat], Long duration [Dexedrine Spansules]; Amphetamine/dextroamphetamine mixture: Short duration [Adderall],Long-duration [Adderall-XR];Methamphetamine [Desoxyn]
Methylphenidate(Ritalin) Used for ADHD, By far, the most commonly used, CNS stimulant, Drug Holidays, summer vacation, Different structure, similar effect to amphetamines
Atomoxetine(Strattera) Selective NE reuptake inhibitor, 1st non-stim approved for ADHD; re-uptake blockade immediate, full therapeutic effects later, not controlled or abusd, 1/day, use in aldults; children: wgt loss, growth retardation, thoughs of suicide
Atomoxetine adverse effects GI reactions, Reduced appetite, Dizziness, Somnolence, Mood swings, Trouble sleeping
Methylxanthines Caffeine: Reversible blockade of adenosine receptors, Calcium permeability, accumulation of cyclic AMP, lower risk of Parkinson, relives headaches
Mehtylzanthines Pharmacologic effets CNS stim, inc heart, dilates periphery constricts CNS, bronchodilation, diuretic, birth deffects; readily absorbed from the GI tract; achieves peak plasma levels within 1 hour, eliminated by hepatic metabolism
Methylxanthines Therapeutic uses Neonatal apnea (Caffeine citrate [Cafcit]), Promoting wakefulness; Theophylline: Bronchodilation, treatment of asthma;
Methylxanthines Acute Toxicity Stimulation of the CNS, Tachycardia, Respiratory stimulation, Sensory phenomena (tinnitus, ‘flashing lights’)
Miscellaneous CNS Stimulants Pemoline (Cylert): Similar to amphetamines, lower cardiac effects, acute liver failure, approved for ADHD; Modafinil (Provigil) Similar to amphetamines, MOA not known, Only approved for narcolepsy, promotes wakefulness
Drug abuse using a drug in a fashion inconsistent with medical or social norms
Drug addiction Disease process characterized by continued use of psychoactive substance(s) despite physical, psychologic, or social harm
Addiction & Drug Abuse Molecular changes in the brain:Reward circuit (system that normally serves to reinforce behaviors essential for survival) is activated; Reinforcing properties of drugs,Physical dependence, Social factors, Drug availability, Vulnerability of the individu
The Controlled Substances Act Comprehensive Drug Abuse Prevention and Control Act of 1970; Record keeping, DEA Schedules I through V, Prescriptions, Labeling, State laws
Basic Pharmacology of Alcohol CNS acute effects: depression of CNS, enhance GABA-mediated inhibition, dose dependant, activation of reward circuit (5ht3 receptors; chronic: Wernicke's emcephalopathy, korsakoff's psychosis, impact on cognitive function; effect on sleep
Alcohol drug interactions CNS depressants, Nonsteroidal anti-inflammatory drugs (GI mucosa), Acetaminophen (liver damage), Disulfiram (Antabuse), Antihypertensive drugs, tolerance and physical dependance
Alcohol Abuse Relapsing disorder, Impaired control over drinking, Preoccupation with alcohol consumption, Use of alcohol despite awareness of adverse consequence, Distortions in thinking, Influenced by genetics, psychosocial, and environmental factors
Drugs Used For Alcohol Withdrawal Benzodiazepines: Diazepam (valium), oxazepam (serax), Lorazepam (ativan); adjuncts to benzodiapines: carbamazepine (antiepileptic drug); clonidine (alpha blocker), atenolo & propanolol (beta blockers)
Drugs Used For Abstinence (alcohol) Disulfiram (Antabuse) aversion therapy: Refrain from drinking, Causes irreversible inhibition of aldehyde dehydrogenase, Causes acetaldehyde syndrome when mixed with alcohol, Patients must be carefully chosenPatients must avoid ALL forms of alcohol,
Naltrexone(Revia) pure opiod antagonist, decrease cravings for alcohol, blocks alcohol's reinforcing effects, mech unclear, adv. nausea and headache
Acamprosate(Campral) Reducing unpleasant feelings abstinence, Devoid of direct anxiolytic, anticonvulsant, and antidepressant activity (? GABA, ? glutamate release?), Does not cause alcohol aversion, Admin orally, Excreted unchanged pee,diarrhea, avoid pregnancy
Drugs Used to Maintain Abstinence Topiramate (Topamax): Reduce craving for alcohol, AED with multiple MOAs; Ondansetron (Zofran): Selective 5-HT3-receptor antagonist