Tranquilizers & Antidepressants Chapter 23 (pg ) Prostaglandins & Inhibitors Chapter 24 (pg )

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) -Ativan (lorazepam) -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) *Geodon (ziprasidone)

- LITHIUM - LITHIUM CARBONATE – highly effective in control of BIPOLAR DISORDER (mechanism-of-action not fully known) ( days for FULL drug effect) * DDI’s (lithium drug interactions …see Table 23-1) Pregnancy Caution: fetal toxicity, especially during 1 st 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 1 st effect in 2 weeks, 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)

Thanks and have a good week!