Sedatives and Hypnotics

Sedatives are a class of drugs that are central nervous system depressants. Hypnotics are drugs that induce sleep, sometimes called soporifics hypnotics are also central nervous system depressants. The term "sedative-hypnotics" refers to a heterogeneous class of drugs that includes benzodiazepines, barbiturates, and various other hypnotics. A sedative lowers excitement and calms the awake patient, whereas a hypnotic produces drowsiness and promotes sleep. By tradition, they are categorized into a single class because of their common ability to induce sedation and sleep. All of these medications when used at usual dosage depress the central nervous system and cause a mild analgesic effect. All drugs in this class can become both psychologically and physically addictive. They also demonstrate a cross-tolerance and potentiation of one another as well as with alcohol which is also a central nervous system depressant.
Indications
Barbiturates and benzodiazepines are the two major categories of sedative-hypnotics. The drugs in each of these groups are similar in chemical structure.
· Barbiturates
1. Short-acting barbiturates are only used for anesthesia induction.
2. Longer-acting barbiturates are used for management of epilepsy and have a role in management of sedative withdrawal; their use for treatment of anxiety and insomnia has largely been replaced by benzodiazepines.
· Benzodiazepines
3. Benzodiazepines are most commonly used for management of anxiety and for insomnia
4. They can also be used for muscle relaxation, sedation/amnesia before medical or surgical procedures, and treatment of epilepsy and seizure states, treatment of alcohol or sedative withdrawal, or acute agitation. They are used intravenously as a component of balanced anesthesia.
5. They have a role in the initial management of acute mania or agitated psychosis, as well as for control of drug-induced hyperexcitable states (eg, stimulant or PCP intoxication).
Tranquilizer
6.induces tranquility in an individual
7.minor tranquilizer usually refers to anxiolytic or antianxiety agent
8.minor tranquilizer usually refers to anxiolytic or antianxiety agent

Sedatives and Hypnotics Generic Names

1. Non-Barbiturates
A. Benzodiazepines
o Estazolam
1. Prozom
Indication
-Indicated for the short-term management of insomnia characterized by difficulty in falling asleep, frequent nocturnal awakenings, and/or early morning awakenings.

Common Side Effects
- Somnolence, hypokinesia, dizziness, and abnormal coordination.

Available Dosage Forms
-Tablet

Contraindications
-ProSom is contraindicated in pregnant women. If there is a likelihood of the patient becoming pregnant while receiving ProSom she should be warned of the potential risk to the fetus and instructed to discontinue the drug prior to becoming pregnant. The possibility that a woman of childbearing potential is pregnant at the time of institution of therapy should be considered.

Pregnancy Category
­-Pregnancy Category X

o Flurazepam
1. Dalmane
Indications
-Dalmane is a hypnotic agent useful for the treatment of insomnia characterized by difficulty in falling asleep, frequent nocturnal awakenings, and/or early morning awakening. Dalmane can be used effectively in patients with recurring insomnia or poor sleeping habits, and in acute or chronic medical situations requiring restful sleep. Sleep laboratory studies have objectively determined that Dalmane is effective for at least 28 consecutive nights of drug administration. Since insomnia is often transient and intermittent, short-term use is usually sufficient. Prolonged use of hypnotics is usually not indicated and should only be undertaken concomitantly with appropriate evaluation of the patient.

Common Side Effects
-Dizziness, drowsiness, light-headedness, staggering, ataxia and falling have occurred, particularly in elderly or debilitated persons. Severe sedation, lethargy, disorientation and coma, probably indicative of drug intolerance or overdosage, have been reported.

Available Dosage Forms
- 15 mg hard gelatin capsules in bottles of 100 (NDC 0187-4051-10), with ICN logo imprinted on the opaque orange cap and Dalmane® 15 imprinted on the opaque ivory body.
-30 mg hard gelatin capsules in bottles of 100 (NDC 0187-4052-10), with ICN logo imprinted on the opaque red cap and Dalmane® 30 imprinted on the opaque ivory body.

Contraindications
- Dalmane is contraindicated in pregnant women. Symptoms of neonatal depression have been reported; a neonate whose mother received 30 mg of Dalmane nightly for insomnia during the 10 days prior to delivery appeared hypotonic and inactive during the first 4 days of life. Serum levels of N1-desalkyl-flurazepam in the infant indicated transplacental circulation and implicate this long-acting metabolite in this case. If there is a likelihood of the patient becoming pregnant while receiving flurazepam, she should be warned of the potential risks to the fetus. Patients should be instructed to discontinue the drug prior to becoming pregnant. The possibility that a woman of childbearing potential may be pregnant at the time of institution of therapy should be considered.
o Quazepam
1. Doral
Indications
- indicated for the treatment of insomnia characterized by difficulty in falling asleep, frequent nocturnal awakenings, and/or early morning awakenings. The effectiveness of DORAL® has been established in placebo-controlled clinical studies of 5 nights duration in acute and chronic insomnia. The sustained effectiveness of DORAL® has been established in chronic insomnia in a sleep lab (polysomnographic) study of 28 nights duration.

Common Side Effects
- Adverse events most frequently encountered in patients treated with quazepam are drowsiness and headache.

Available Dosage Forms
- DORAL® Tablets, 7.5 mg, unscored, capsule-shaped, light orange, slightly white speckled tablets, impressed with the product identification number 7.5 on one side of the tablet, and the product name (DORAL) on the other.
7.5 mg Bottles of 100 NDC 63004-7735-1
DORAL® Tablets, 15 mg, unscored, capsule-shaped, light orange, slightly white speckled tablets, impressed with the product identification number 15 on one side of the tablet, and the product name (DORAL) on the other.
15 mg Bottles of 100 NDC 63004-7734-1

Contraindications
- DORAL® Tablets are contraindicated in patients with known hypersensitivity to this drug or other benzodiazepines, and in patients with established or suspected sleep apnea.

Preganancy Category
- Pregnancy Category X


B.
Non-Benzodiazepines
o Zolpidem
1. Ambien
Indications
- Ambien (zolpidem tartrate) is indicated for the short-term treatment of insomnia characterized by difficulties with sleep initiation. Ambien has been shown to decrease sleep latency for up to 35 days in controlled clinical studies

Common Side Effects
- Dizziness, lightheadedness, headache, upset stomach, diarrhea, and dry mouth may occur.

Available Dosage Forms
- Ambien is available in 5 mg and 10 mg strength tablets for oral administration. Tablets are not scored.
Ambien 5 mg tablets are capsule-shaped, pink, film coated, with AMB 5 debossed on one side and 5401 on the other.
Ambien 10 mg tablets are capsule-shaped, white, film coated, with AMB 10 debossed on one side and 5421 on the other.

Contraindications
- Ambien is contraindicated in patients with known hypersensitivity to zolpidem tartrate or to any of the inactive ingredients in the formulation. Observed reactions include anaphylaxis and angioedema

Preganancy Category
-Pregnancy Category C


o Chloral Hydrate
1. Noctec
Indications
- Chloral hydrate is indicated for nocturnal sedation in all types of patients and especially for the ill, the young, and the elderly patient.
-In candidates for surgery, it is a satisfactory preoperative sedative that allays anxiety and induces sleep without depressing respiration or cough reflex. In postoperative care and control of pain, it is a valuable adjunct to opiates and analgesics.

Common Side Effects
- Occasionally a patient becomes somnambulistic and he may be disoriented and incoherent and show paranoid behavior. Rarely, excitement, tolerance, addiction, delirium, drowsiness, staggering gait, ataxia, lightheadedness, vertigo, dizziness, nightmares, malaise, mental confusion and hallucinations have been reported.
Available Dosage Forms
- Chloral Hydrate Syrup, USP is supplied as a clear, pink to orange colored, orange flavored syrup containing 500 mg (7½ gr) in 5 mL (teaspoonful) in the following size:
16 fl oz (473 mL)

Contraindications
- Chloral hydrate is contraindicated in patients with marked hepatic or renal impairment and in patients with severe cardiac disease. Oral dosage forms of chloral hydrate are contraindicated in the presence of gastritis. Chloral hydrate is also contraindicated in patients who have previously exhibited an idiosyncrasy or hypersensitivity to the drug.
Preganancy Category
- Category C


2. Barbiturates

o Phenobarbital
  1. Nembutal
Indications
- Parenteral
a. Sedatives.
b. Hypnotics, for the short-term treatment of insomnia, since they appear to lose their effectiveness for sleep induction and sleep maintenance after 2 weeks (See "CLINCAL PHARMACOLOGY" section).
c. Preanesthetics.
d. Anticonvulsant, in anesthetic doses, in the emergency control of certain acute convulsive episodes, e.g., those associated with status epilepticus, cholera, eclampsia, meningitis, tetanus, and toxic reactions to strychnine or local anesthetics.

Common Side Effects
- Nervous system: Agitation, confusion, hyperkinesia, ataxia, CNS depression, nightmares, nervousness, psychiatric disturbance, hallucinations, insomnia, anxiety, dizziness, thinking abnormality.
Respiratory system: Hypoventilation, apnea.
Cardiovascular system: Bradycardia, hypotension, syncope.
Digestive system: Nausea, vomiting, constipation.
Other reported reactions: Headache, injection site reactions, hypersensitivity reactions (angioedema, skin rashes, exfoliative dermatitis), fever, liver damage, megaloblastic anemia following chronic phenobarbital use.

Available Dosage Forms
- NEMBUTAL Sodium Solution (pentobarbital sodium injection, USP) is available in the following sizes:
20-mL multiple-dose vial, 1 g per vial (NDC 67386-501-52); and 50-mL multiple-dose vial, 2.5 g per vial (NDC 67386-501-55).

Contraindications
- Barbiturates are contraindicated in patients with known barbiturate sensitivity. Barbiturates are also contraindicated in patients with a history of manifest or latent porphyria.

Preganancy Category
- Pregnancy Category D


o Mephobarbital
  1. Mebaral
Indications
- MEBARAL is indicated for use as a sedative for the relief of anxiety, tension, and apprehension, and as an anticonvulsant for the treatment of grand mal and petit mal epilepsy.

Common Side Effects
- Drowsiness, dizziness, upset stomach, or headache may occur. If any of these effects persist or worsen, notify your doctor or pharmacist promptly.
Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.


Available Dosage Forms
- Tablets—white, round, convex and the 32 mg and 50 mg tablets are scored.
32 mg (½ grain), bottles of 250 (NDC 67386-801-02).
50 mg (3/4 grain), bottles of 250 (NDC 67386-802-02).
100 mg (1 ½ grains), bottles of 250 (NDC 67386-803-02).

Contraindications
- Hypersensitivity to any barbiturate. Manifest or latent porphyria.
Preganancy Category
- Pregnancy Category D

o Butabarbital Sodium
  1. Butisol
Indications
- is indicated for use as a sedative or hypnotic.

Common Side Effects
- Unwanted sleepiness and trouble waking up in the morning may occur. Less common side effects may include headache, constipation, nausea, vomiting, nightmares, and increased dreaming.

Available Dosage Forms
- BUTISOL SODIUM® (butabarbital sodium tablets, USP):
30 mg - colored green, scored, imprinted “BUTISOL SODIUM” and 37/113 in bottles of 100 (NDC 0037-0113-60).
50 mg - colored orange, scored, imprinted “BUTISOL SODIUM” and 37/114 in bottles of 100 (NDC 0037-0114-60).
BUTISOL SODIUM® (butabarbital sodium oral solution, USP): 30 mg/ 5 mL, alcohol (by volume) 7% - colored green, in bottles of one pint (NDC 0037-0110-16).

Contraindications
- Barbiturates are contraindicated in patients with known barbiturate sensitivity. Barbiturates are also contraindicated in patients with a history of manifest or latent porphyria.

Preganancy Category
-Pregnancy Category D




Apostol, Bonn Kevin
Choy-awon, Crispina
Joaquin, Jennifer
Kitong, Agnetha

3:00-4:00 MWF
81/100 - only one brand for each instead of three