Pharm 1 Final (Anxyolitic)

Naloxone (Narcan) Adverse effects

Adverse effects Respiratory depression is the most serious adverse effect associated with opioids. • Stimulating the patient may be adequate to reverse mild hypoventilation. •If this is unsuccessful, ventilatory assistance using a bag and mask or endotracheal intubation may be needed to support respiration. •Failure of the drug to signifcantly reverse the effects of the presumed opioid overdose indicates that the condition may not be related to opioid overdose. •The primary adverse effect is opioid withdrawal syndrome, which can occur with abrupt overreversal in opioid-tolerant patients.

Benzodiazepine MOA

Benzodiazepines Reduce overactivity in the CNS (all anxiolytics- not just Benzodiazepines) Exert maximal effects in the areas of the brainstem limbic system Increases GABA - an inhibitory neurotransmitter which inhibits nerve transmission in the CNS Produces skeletal muscles relaxation & sedation Anticonvulsant properties

Benzodiazepine

Benzodiazepines (most commonly prescribed) for the treatment of anxiety

ANTIDOTE for anxyolitics

Flumazenil (Romazicone)

Benzodiazepine Different Medications?

Chlordiazepoxide (Librium) Clonazepam (Klonopin) Diazepam (Valium) prototype Oxazepam (Serax) Clorazepate (Tranxene) Lorazepam (Ativan) Alprazolam (Xanax) Yellow should be used short term chart on next slide

Benzo Caution

Dependence Tolerance Physical addiction Psychological addiction Withdrawal syndrome Xanax, Valium, and Ativan should only be used short-term. Dependence and tolerance develop quickly. Signs and symptoms of withdrawal Anxiety, tremors, insomnia Grand mal seizures, delirium Respiratory depression and death

SIDE EFFECTS OF ANXIOLYTICS

Excessive sedation Hypotension Paradoxical excitement Chronic intoxication

Naloxone Indications, Route

For severe respiratory depression, opioid antagonists (naloxone) may be used to improve respiratory status and, if they are titrated in small amounts, the respiratory depression may be reversed without analgesia reversal. • is a pure opioid antagonist. •It has no agonistic morphine-like properties and works as a blocking drug for the opioid drugs. •Does not produce analgesia or respiratory depression. •drug of choice for the complete or partial reversal of opioid- induced respiratory depression. •indicated in cases of suspected acute opioid overdose. Route • Naloxone is available only in injectable dosage forms. Use of the drug is contraindicated in patients with a history of hypersensitivity to it.

Lorazepam (Ativan) Onset of action, duration of action, route, Indications

Onset of Action: 30-60 Minutes Duartion of action: 8 hours •intermediate-acting benzodiazepine. alprazolam is the shortest acting, whereas diazepam is the longest acting. Route •Lorazepam is available in oral and injectable forms. •It may be given intravenously or intramuscularly. •It has excellent absorption and bioavailability when given intramuscularly, but it is irritating to the muscle and must be diluted. The conversion between injectable and oral dosage forms is 1:1. Indications •Lorazepam can be given by intravenous push, which is useful in the treatment of an acutely agitated patient. • It is often administered as a continuous infusion to agitated patients who are undergoing mechanical ventilation. It is also used to treat or prevent alcohol withdrawal. Indications, contraindications, and adverse effects are similar to those of alprazolam.

Anxiolytic patient teaching

Routine oral dosing given at bedtime Avoid alcohol and caffeine Caution against driving and operating machinery Do not stop abruptly Report sleep pattern changes Paradoxical excitation Observe for therapeutic effects Observe for adverse effects

Benzodiazepine Indications for use:

Short term treatment of anxiety Treatment of seizure disorder Useful in the acute stage of panic Insomnia Alcohol withdrawal commonly used as adjunct therapy for depression because depressive and anxious symptoms often occur together. •sedation •relief of agitation or anxiety, •treatment of anxiety-related depression, sleep induc-tion, skeletal muscle relaxation, and treatment of acute seizure disorders. •Benzodiazepines are often combined with anesthet- ics, analgesics, and neuromuscular blocking drugs in balanced anesthesia and also moderate sedation for their amnesic properties to reduce memory of painful procedures. •benzodiazepine receptors in the CNS are in the same area as those that play a role in alcohol addiction. Therefore, some benzodiazepines (e.g., diazepam,) are used in the treatment and prevention of the symptoms of alcohol withdrawal. •when treating insomnia, it is recommended to be used short term if feasible to avoid dependency.

Diazepam (Valium) Trade name, duration of action, Contraindications, Adverse Effects, Interactions

Trade Name (Valium) diazepam is the longest acting. Contraindications •has active metabolites that can accumulate in patients with hepatic dysfunction, because it is metabolized primarily in the liver. resulting in additive, cumulative effects that may be manifested as prolonged sedation, respiratory depression, or coma. •avoided in patients with major hepatic compromise. Adverse Effects •Adverse drug effects include headache, confusion, slurred speech, and others listed in Table 16-2. Interactions Diazepam interacts with alcohol, oral contraceptives, and others as shown in Table 16-3. Diazepam is available in oral, rectal, and injectable dosage forms.

Diazepam Indications

most commonly prescribed benzodiazepine •for treatment of anxiety, it has generally been replaced by the shorter-acting benzodiazepines alprazolam and lorazepam. •indicated for the relief of anxiety, management of alcohol withdrawal, reversal of status epilepticus, preoperative sedation, and occasionally for relief of skeletal muscle spasms.

Anxiolytics Nursing Considerations

prescriber may order laboratory studies, such as complete blood counts, serum electrolyte levels, and hepatic/renal function studies (see earlier discussion). Blood pressure readings are also very important to assess because of drug-related postural hypotension. The baseline neurologic examination needs to include assessment of alertness, orientation, and sensory/motor functioning as well as any complaints of ataxia, headache, or other neurologic abnormalities.

alprazolam Trade name, Indications, adverse effects,

trade Name Alprazolam (Xanax) • is most commonly used as an anxiolytic. indicated for the specific anxiety disorder known as panic disorder. Adverses effects include confusion, ataxia, head- ache, and others listed in Table Interactions • Interacting drugs include alcohol, antacids, oral contraceptives, and others listed in Table 16-3. Alprazolam is available only for oral use, in both tablet and orally dissolving tablet forms. The orally dissolving tablet is indicated for the treatment of anxiety disorder, short-term relief of anxiety symptoms, treatment of anxiety associated with depression, and treatment of panic disorder with or without agoraphobia.

naloxone Trade name, MOA, Indications

trade name Narcan MOA •Naloxone and naltrexone are opioid antagonists, and they bind to and occupy all of the receptor sites (mu, kappa, delta). •They are competitive antagonists with a strong affinity for these binding sites. •Through such binding they can reverse the adverse effects induced by the opioid drug, such as respiratory depression. Indications •These drugs are used in the management of both opioid overdose and opioid addiction. The commonly used opioid antagonists (reversal drugs) are listed in Table 10-7.

alprazolam Interactions, Route

• Interacting drugs include alcohol, antacids, oral contraceptives, and others listed in Table 16-3. Route Alprazolam is available only for oral use, in both tablet and orally dissolving tablet forms. The orally dissolving tablet is indicated for the treatment of anxiety disorder, short-term relief of anxiety symptoms, treatment of anxiety associated with depression, and treatment of panic disorder with or without agoraphobia.

Benzodiazepine Interactions

•Alcohol and CNS depressants, when coad- ministered with benzodiazepines, can result in additive CNS depression and even death. This serious consequence is more likely to occur in patients with renal and/or hepatic compro- mise (e.g., the elderly). Other drug interactions are listed in Table 16-3.

Benzodiazepine Contraindications

•Contraindications to benzodiazepines include known drug allergy; •narrow-angle glaucoma, due to their ability to cause mydriasis(dilation of the pupil of the eye); and •pregnancy, due to their sedative properties and risk for teratogenic effects.

Naloxone Nursing Consideratinos

•When treating an opioid overdose or toxicity, the symptoms of withdrawal need to be considered. •regardless of potential withdrawal symptoms, when a patient experiences severe respiratory depression, naloxone must be given. • Some degree of physical dependence is expected in opioid-tolerant patients. •The extent of opioid tolerance is most visible when an opioid drug is discontinued abruptly or when an opioid antagonist is administered. This usually leads to symptoms of opioid withdrawal, also known as abstinence syndrome • This can occur after as little as 2 weeks of opioid therapy in opioid-naïve patients. •Gradual dosage reduction after chronic opioid use, when possible, helps to minimize the risk and sever- ity of withdrawal symptoms. Administration of opioid antagonists (e.g., naloxone) may also be necessary to reverse severe respiratory depression. •Careful titration of dose until the patient begins to breathe independently will prevent over-reversal. •The effects of naloxone are short lived and usually last about 1 hour. With long-acting opioids, respiratory depressant effects may reappear, and naloxone may need to be re-dosed.

Benzodiazepine Adverse Effects?

•overexpression of their therapeutic effects, in particular •CNS depression. •hypotension. paradoxical reactions (opposite of those that would normally be expected) e.g., hyperactivity and aggressive behav-ior. •Rebound disinhibition can occur in elderly patients upon tapering of doses or discontinuation of the benzodiazepines. an elderly patient experiences marked sedation for 1 to 2 hours, followed by marked agitation and confusion for several hours afterward. potentially habit-forming and addictive (Schedule IV). Although they can provide significant symptom relief, they must be used judiciously and at the low- est effective doses needed for symptom control. See Table 16-2 for more information on adverse effects. Elderly patients more sensitive to the sedating effects of benzodiazepines increasing risk for falls; thus lower doses are usually needed. can be harmful if given in excessive doses or when mixed with alcohol. Adverse effects involve the CNS. Commonly reported undesirable effects are headache, drowsiness, paradoxical excitement or nervousness, dizziness or vertigo, cognitive impair- ment, and lethargy. Benzodiazepines can create a significant fall hazard in elderly patients, and the lowest effective dose must be used in this patient population. Although these drugs have comparatively less intense effects on the normal sleep cycle, a "hangover" effect is sometimes reported (e.g., daytime sleepi- ness). Withdrawal symptoms such as rebound insomnia ( greater insomnia than pretreatment) may occur with abrupt discontinuation.