Pharmacology 2 Exam 1

Benzodiazepine drugs include:

• Alpralozam (Xanax)

• Clonazepam (Klonopin)

• chlordiazepoxide (Librium)

• Diazepam (Valium)

• Lorazempam (Ativan)

• Temazepam (Restolril)

• MEMORY TRICK “PAM”

Which Benzodiazepine can treat alcohol withdrawal symptoms?

chlordiazepoxide (Librium)

What is the action of a Benzodiazpeine?

• acts in the limbic system and the RAS

• make GABA more effective

what do lower doses of benzodiazepines assist with?

anxiety

what do higher doses of benzodiazepines assist with?

sedation and hypnosis

what are the indications of Benzodiazepines?

• anxiety disorders

• alcohol withdrawal

• hyper-excitability and agitation

• preoperative relief of anxiety (aids in balanced anesthesia)

• seizure control

Benzodiazepines pharmacokinetics

• well absorbed from GI tract

• peak in 30 minutes - 2 hours

• lipid soluble and distributes well throughout the body

• cross placenta

• enter breast milk

• METABOLIZED IN LIVER

• EXCRETION PRIMARILY IN URINE

Benzodiazpeines contraindications/cautions

• allergy

• psychosis

• acute narrow angle glaucoma

• shock

• coma

• acute alcohol intoxication

• pregnancy

Why are Benzodiazepines contraindicated in pregnancy?

cause cleft palette in the baby

what are the adverse effects of benzodiazepines?

• sedation

• drowsiness

• depression

• lethargy

• blurred vision

• confusion

• dry mouth

• constipation

• n/v

• hypotension

• urinary retention

Benzodiazpines drug-drug interactions

• increases CNS depression when taken with alcohol

• increase in effects when take with cimetidine, oral contraceptives, or disulfiram

• decrease in effects when given with theophylline/rantidine

A patient overdoes on Benzodiazepines what would you as the nurse administer?

Flumazenil (Romazicon)

A patient overdoses on narcotics what would you as the nurse administer?

narcan/naloxone

what is the action of barbiturates?

• CNS DEPRESSANTS

• inhibit neuronal impulse conduction in ascending RAS

• depress cerebral cortex

• depress motor output

what are the names of some Barbiturates?

• Amobarbital

• Butabarbital

• Phenobarbital

• Primidone

MEMORY TRICK “BARBITAL”

Barbiturates indication

• relief of the signs and symptoms of anxiety

• sedation

• Insomnia

• Preanesthesia

• seizures

Barbiturates pharmacokinetics

• well absorbed

• PEAK 20-60 minutes

• METABOLIZED IN LIVER

• EXCRETED IN URINE

Barbiturates contraindications and cautions

• Allergy: give IV benadryl

• marked hepatic impairment or nephritis

Barbiturates adverse effects

• CNS Depression

• Physical Dependency

• Drowsiness

• Somnolence

• Lethargy

• Ataxia

• Vertigo

• Nausea

• Vomiting

• Constipation

Barbiturates drug-drug interactions

• increase CNS DEPRESSION when given with alcohol, antihistamines, other tranquilizers

• altered respone to phenytoin

• MAOI cause increase serum levels and effect

which specific class of drugs can Barbiturates effect?

• anticoagulants

• digoxin

• triycyclic antidepressants

• cotricosteroids

• oral contraceptives

What is the preferred anxiolytic drug ?

Buspirone (Buspar): reduces the s/s of anxiety WITHOUT severed CNS and adverse effects

NOT ADDICTING

what are 3 other anxiolytic and hypnotic drugs?

• antihistamines: promethazine (promethegan), diphenhydramine

• dexmedetomidine (precedex)

• Eszopiclone (lunesta)

what are some s/s of depression?

• low energy level

• sleep disturbances

• lack of appetite

• limited libido

• inability to perform ADLs

• overwhelming feelings of sadness, despair, hopelessness, and disorganization

what respiratory disorder puts patients at high risk of depression?

copd

what are the actions of antidepressant therapy?

inhibit the effects of MAO

Monoamine oxidase (MAO)

may break them down to be recycled or restored in the neuron

what are the 4 classifications of antidepressants?

• tricylic antidepressants (TCAs)

• MAO inhibitors (MAOIs)

• selective serotonin reuptake inhibitors (SSRIs)

• serotonin norepinephrine inhibitors (SNRIs)

what are the 3 trycylic antidepressants?

• Imipramine

• Amitriptyline

• Notriptyline

what is the action of trycyclic antidepressants?

reduce the reuptake of 5HT (serotonin) and NE into nerves

indications of tricyclic antidepressants

• relief of symptoms of depression

• used in pts. with sleep disorders

• treatment of enuresis

• chronic pain

pharmacokinetics of trycyclic antidepressants

• peak 2-4 hours

• T 1/2 8-46 hours

• metabolized in the liver

• excreted in the urine

contraindications of trycyclic antidepressants (TCA)

• known allergy

• recent MI

• Myelography

• PREGNANCY AND LACTATION

TCA cautions

Cv disease, angle closure glaucoma, urinary retention, manic-depression

MONITOR URINE OUTPUT

TCA drug-drug interactions

MAOIs, cimetidine, fluoxetine, ranitidine, oral anticoagulants

TCA adverse effects

• sedation

• sleep disturbances

• fatigue

• hallucinations

• ataxia

• dry mouth

• constipation

• N/V

Monoamine Oxidase Inhibitors examples:

• Isocarboxazid (Marplan)

• Phenelzine (Nardil)

• Tranycypromie (parnate)

• MEMORY TRICK MAR, NAR, PAR!!!!!!

Isocarboxazide (Marplan) (MAOIs) used for ?

patients who did not respond to or could not take newer safer antidepressants

Phenelzine (Nardil) (MAOIs) used for?

patients who did not respond to newer safer antidepressants

Tranylcypromine (Partite) (MAOIs) used for?

adult outpatients with reactive depression

MAOIs action?

irreversibly inhibits MAO allowing epinephrine, serotonin, and dopamine to accumulate in the synaptic cleft

indications of MAOIs

treatment of patients with depression who are unresponsive or unable to take other antidepressants

MAOIs pharmacokinetics

• absorbed from GI tract

• peak 2-3 hours

• metabolized in the liver, excreted in the urine

• cross placenta and enter breast milk

MAOIs contraindications

• known allergy

• pheochromocytoma

• CV disease

• headaches

• RENAL OR HEPATIC IMPAIRMENT

MAOIs adverse effects

• dizziness

• excitement

• nervousness

• mania

• hyperreflexia

• tremors

• confusion

• insomnia

• agitation

• liver toxicity

• N/V

• diarrhea or constipation

• anorexia

• weight gain

• dry mouth

• abdominal pain

MAOIs drug interactions

• other antidepressants

• methyldopa

• insulin or oral anti diabetic agents

MAOIs food interactions

tyramine or pressor amine = increase BP

selective serotonin repute inhibitors (SSRIs)

specifically block the rep uptake of 5HT (serotonin) with little to no effect on NE

what is the benefit of SSRIs?

do not have many adverse effects associated with TCAs and MAOIs

indications of SSRIs

• depression

• OCDs

• panic attacks

• bulimia

• premenstrual dysmorphic disorder

• PTSD

• social phobias

• social anxiety

SSRIs pharmacokinetics

• absorbed from GI tract

• metabolized in liver

• associated with congenital abnormalities

SSRIs contraindications

• known allergy

• pregnancy and lactation

• impaired renal or hepatic function

SSRIs adverse effects

• headache

• drowsiness

• dizziness

• INSOMNIA

• anxiety

• tremor

• agitation

SSRIs drug interactions

• MAOIs

• TCAs increase therapeutic and toxic effect

SSRI drugs include:

• Fluoxetine (Prozac)

• Paroxetine (Paxil)

• Sertraline (Zoloft)

• Citalopram (Celexa)

• Escitalopram (Lexapro)

Serotonin Norepinephrine inhibitors (SNRIs) actions

decreases neuronal reuptake of both serotonin and norepinephrine and more weakly inhibit dopamine

SNRIs contraindications

• allergies

• MAOIs use

SNRIs adverse effects

• nausea

• constipation

• higher HR

• hyperhidrosis

• erectile dysfunction

• tachycardias

• vomiting

• palpations

• serotonin syndrome

• HTN

• abnormal bleeding

• angle closure glaucoma

• urinary retention

SNRIs drug-drug interactions

• MAOIs

• SSRIs

• TCAs

• serotonergic drugs

• aspirin

• NSAIDs

• antiplatelet drugs

SNRIs include:

• Desvenlafazine (Pristiq)

• Duloxetine (Cymbalta)

• Levomilnacipran (Fetzima)

• Venlafaxine (Effexor, Effexor XR)

what drug helps with suicide and smoking cessation ?

Bupropion (Wellbutrin, Zyban)

psychotherapeutic agents

• used to treat psychoses

• DRUGS DO NOT CURE THE DISORDER

• used in both children and adults

• HELPS PT. FUNCTION

scihizophrenia

hallucination, paranoia, delusions, speech abnormalities, and effective problems

what are the causes of schizophrenia?

• strong genetic association

• may reflect a fundamental biochemical abnormality

antipsychotic/neuroleptic drugs actions

• block dopamine receptors, preventing the stimulation of the postsynaptic neurons by dopamine

• depress RAS, limit stimuli coming to brain

what are the indications for antipsychotic/neuroleptic drugs?

• schizophrenia

• hyperactivity

• combative behavior

• agitation in elderly

• severe behavioral problems in children

antipsychotic/neuroleptic drugs contraindications

• underlying diseases that could be exacerbated by dopamine-blocking effects of these drugs

• CNS depression

• Parkinson’s disease

• prolonged QT interval

antipsychotic/neuroleptic drugs include:

• haloperidol (Haldol)

• chlorpromazine (Thorazine)

  • POOR COMPLIANCE WITH THESE MEDS

drugs for bipolar disorders include:

• Lithium (Lithobid)

• Apripiprazole (Abilify)

• Lamotrigine (Lamictal)

• Olanzapine (Zyprexa)

• Quetiapine (Seroquel)

• Ziprasidone (Geodon)

actions of lithium

• alters sodium transport in nerve and muscle cells

• inhibits release of NE and dopamine but not serotonin

• increases intraneuronal stores of NE and dopamine slightly

adverse effects of lithium

• <1.5 = lethargy, slurred speech, weakness, N/V

• 1.5-2 = above plus ECG changes

• 2-2.5 = ataxia, hyperreflexia

• 2.5 = DEATH

lithium pharmacokinetics

• peak in 30 minutes

• excreted from kidneys 80% reabsorbed

CNS stimulants actions

act as cortical and RAS, increase release of catecholamines leading to increased stimulation of the postsynaptic neurons

CNS stimulants indications

• attention deficit disorder/syndromes

• narcolepsy

CNS stimulants pharmacokinetics

• peak 2-4 hours

• T 1/2 2-15 hours

what is an example of a CNS stimulant?

Methylphenidate (Ritalin)

nursing considerations = tolerance and dose, may be habit forming, insomnia, and heart defect

anti seizure agents include: HYDANTOINS

Hydantoins

• Ethotoin (Peganone)

• Fosphenytoin (Cerebryx)

• Phenytoin (Dilantin)

therapeutic serum phenytoin levels

10-20 mcg/mL

therapeutic serum ethotoin levels

15-50 mcg/mL

Hydantoins contraindications and cautions include:

• known allergies

• pregnancy and lactation

• GINGIVAL HYPERLPLASIA

Hydantoins adverse effects

• relate mostly to CNS depression

• sever liver toxicity and bone marrow suppression

hydantoins drug-drug interactions

alcohol

barbiturates and barbiturate-like drugs include:

• phenobarbital (Solfoton, Luminal)

• Primidone (Mysoline)

• phosphenytoin

• ASSOCIATED WITH SIGNIFICANT CNS DEPRESSION

some benzodiazepines are used as anti epileptic drugs such as:

• Clobazam (Onfi)

• Clonazepam (Klonopin)

• Diazepam (Valium)

pharmacokinetics of Benzodiazepines

long half-life of 18-50 hours!!!!

Succinimides indications

most frequently used to treat absence or focal seizures

Succinimides include:

Ethosuximiden (Zarontin)

Methsuximide (Celontin)

MEMORY TRICK SUCC = SUX

contraindications of Succinimides

patients with intermittent porphyria (blood disease)

Succinimides adverse effects

• CNS depressant effects

• BONE MARROW SUPPRESSION

Succinimides drug-drug interactions

Primidone

what are the 2 other drugs for treating absent seizures?

• Acetazolamide (Diamox)

• Valproic acid (Depakene)

Parkinson’s disease

• progressive neuro disorder

• NO CURE

• therapy aimed in management of signs and symptoms

progression of Parkison’s disease

• rhythmic tremors

• rigidity/weakness

• MASK-LIKE FACIAL EXPRESSIONS

• drooling and affected speech

Dopaminergic drugs are for what only?

Parkinson’s disease

contraindications of dopaminergic drugs

• allergy

• angle closure glaucoma

• BPH (benign prostatic hypertrophy): may not be able to pee

dopaminergic adverse effects include:

• anxiety

• nervousness

• headache

• blurred vision

• ARRYTHMIAS!!!!!

Dopaminergics drug-drug interactions

• MAOIs

• Vitamin B6

• Tyramine containing foods

• St. John’s wort

• analgesics

what is the only Dopaminergic drug for parkinson’s ?

Levodopa

what is almost always given in combination with Levodopa?

Carbidopa (Sinemet) because it decreases the amount of levodopa needed to reach therapeutic levels which reduces adverse side effects

Dopaminergic: levodopa drug-drug interactions

• MAOIs = enhances effects of Levodopa

• Vitamin B6