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Tranquilizers & Antidepressants Prostaglandins & Inhibitors. * Chapter 23 (pg 131-140) * Chapter 24 (pg 141-145). TRANQUILIZERS. PURPOSE: to calm or ‘tranquilize’ without excessive sedation or interference with daily function General Categories: *BENZODIAZEPINES
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Tranquilizers & AntidepressantsProstaglandins & Inhibitors * Chapter 23 (pg 131-140) * Chapter 24 (pg 141-145)
TRANQUILIZERS • PURPOSE: to calm or ‘tranquilize’ without excessive sedation or interference with daily function • General Categories: *BENZODIAZEPINES *ANTIPSYCHOTICS *‘OTHER’ sedating agents
BENZODIAZEPINES • MID-level “anxiolytics” and sedatives • “Anxio-lytic” means “to break down anxiety” • Benzo’s are known for their … *Low abuse potential *Low toxicity in overdose (fairly safe drug) • Xanax (alprazolam) • Valium (diazepam) • Klonopin (clonazepam)
ANTIPSYCHOTICS • PHENOTHIAZINES – generally used for the symptomatic management of SEVERE psychiatric disorders (schizophrenia, psychosis) *chlorpromazine *prochlorperazine • NON-PHENOTHIAZINES – severe schizophrenia *Abilify (aripiprazole) *Seroquel (quetiapine) *Zyprexa (olanzapine)
- LITHIUM - • LITHIUM CARBONATE – highly effective in control of BIPOLAR DISORDER • (mechanism-of-action not fully known) • (6 - 10 days for FULL drug effect) * • DDI’s (lithium drug interactions …see Table 23-1) • Pregnancy Caution: fetal toxicity, especially during 1st trimester … must carefully monitor blood levels if lithium use is essential in patient
other SEDATING agents • meprobamate * depresses nerve impulse transmission in spinal-cord and brain * relaxes skeletal muscles, relieves anxiety and tension • Rozerem (ramelteon) * for insomnia of delayed sleep onset * NOT habit-forming (not a controlled substance)
ANTIDEPRESSANTS Types of Depression … • ENDOGENOUS – ‘from within’ has no apparent external cause, tends to be longer-term * responds poorly to drug therapy • EXOGENOUS – associated with traumatic events such as major-illness, loss of loved one * responds very well to drug therapy!
SSRI’S “SELECTIVE SEROTONIN REUPTAKE INHIBITORS” • these result in higher concentrations of available SEROTONIN in the CNS • 1st effect in 2weeks, FULL effect in 4 to 8 weeks --------Celexa (citalopram) --------Lexapro (escitalopram) --------Prozac (fluoxetine) --------Zoloft (sertraline)
MAOI’S MONOAMINE OXIDASE INHIBITORS • Effective antidepressants, but with an extremely high number of both FOOD and DRUG interactions! • Common foods such as … cheese, wine, red meats, liver, avocado (anything w/ tyramine) * Nardil (phenelzine) * Parnate (tranylcypromine)
TCA’S • TRICYCLIC ANTIDEPRESSANTS – ‘tricyclic’ refers to these drugs’ chemical structure • Older group of agents, used many years • Used for insomnia, nerve pain ---------- Elavil (amitriptyline) ---------------- Norpramine (desipramine) -------------------------- Tofranil (imipramine)
- OTHER ANTIDEPRESSANTS - • Wellbutrin (bupropion) • Remeron (mirtazapine) • Serzone (nefazodone) • Effexor (venlafaxine)
NON-PSYCHIATRIC uses of ANTIDEPRESSANTS • May help many patients cope with pain … probably due to increased levels of Serotonin and Norepinephrine • Used prophylactically for MIGRAINE headaches, PREMENSTRUAL syndrome, and neuralgias
ANXIOLYTIC’S • ANXIOLYTICS relieve anxiety, and are generally less sedating than the Tranquilizers • Better choice for long-term use because of significantly fewer side-effects • BUSPAR (buspirone) primary agent this class • The term ‘anxiolytic’ is often used generally for any and all drugs that can relieve anxiety … from Xanax to Benadryl!
ANTICONVULSANTS in Anxiety • Anticonvulsants are being used to treat anxiety disorders, as well as PTSD (Post Traumatic Stress Disorder) • Tegretol (carbamazapine) • Depakote (divalproex) • Neurontin (gabapentin) • Topamax (topiramate)
---- PROSTAGLANDINS (PG’s) ----- • Physiologically ‘active’ substances found in many of the body’s tissues • For example, Aspirin has its effect by altering the PROSTAGLANDIN system • They are name as follows … prostaglandin-A = ‘PGA’ prostaglandin-B = ‘PGB’, and so on
PG: ACTIONS by Body system • REPRODUCTIVE TRACT – Prostin E2 suppositories • CIRCULATORY SYSTEM – alprostadil IV pediatric • GASTROINTESTINAL TRACT – Cytotec (misoprostol) • URINARY TRACT – MUSE (alprostadil) for E.D. (ouch!) • IMMUNE SYSTEM/ALLERGY RESPONSE – no drugs have yet been developed that can predictably manipulate the allergic/immune response
PG Inhibitors • A ‘Prostaglandin-inhibitor’ is any agent that exerts its effect by blocking or interfering with the normal function of one of the prostaglandin systems • MOA of most is the interruption of prostaglandin synthesis at the site of the inflammation (example, the NSAID’s)
NSAID’S • As previously mentioned, these drugs act by reducing prostaglandin synthesis at the site of inflamed tissue ----ASPIRIN ------Voltaren (diclofenac) --------Motrin, Advil (ibuprofen) ----------Mobic (meloxicam) ------------Feldene (piroxicam)
COX-2 INHIBITORS • MAJOR ADVANTAGE is these specifically block only the COX-2 enzyme • NSAID’s block both COX-1 and COX-2 which has negative effects on the stomach-lining, resulting in ulcer-formation & bleeding --------- Celebrex (celecoxib)