Central stimulants, benzodiazepine antagonists, puzzlers

  Name
  Specification and Packaging
  Properties, usage and side effects
  1
  Methylphenidate, trade name Ritalin Ritalin
  10mg*20
  (Class I psychotropic drug, limited to 40 tablets)
  Heterocyclic sympathomimetic drugs. It is a stimulant, with a slight increase in heart rate and elevated blood pressure. Used for mental fatigue, episodic sleeping sickness, attention deficit disorder, etc., as well as central depressant-induced drowsiness. The methylphenidate test is used as a differential diagnosis between depressive subtypes and other psychiatric disorders. It is easily absorbed orally, T1/2 about 2h, excreted by urine, and acidic urine promotes excretion. Oral dose 5-10mg/d, 1~2 times/d, usually no later than 4:00 p.m. Children over 6 years old start at 5mg/d and increase by 5-10mg/d every other week depending on the situation. total daily dose not more than 20mg under 12 years old, 30mg over 12 years old. maximum 60mg/d. For the treatment of attention deficit disorder, a “drug holiday” system is required to prevent growth suppression. In order to prevent the suppression of growth, a “drug holiday” system should be adopted, i.e., the drug should be stopped during weekends and summer and winter vacations.
  Adverse effects are rare, occasionally tachycardia, headache, insomnia, excitement, anxiety, epigastric discomfort, anorexia, etc. A few children can induce twitching symptoms. May inhibit height growth. Cannot be used with MAOI. Contraindicated in patients with glaucoma, epilepsy, hypertension and overexcitement. It has euphoric effect and can cause dependence in long-term use.
  2
  Clonidine, alias Clonidine Clonidine
  0.0375mg*100
  0.075mg*100
  Alpha 2 agonist, a central antihypertensive drug. It is mainly used for hypertension, but also has anti-epileptic, sedative and hypnotic effects. It can stimulate the secretion of growth hormone, inhibit atrial fluid formation and lower intraocular pressure. It is used to relieve the sympathetic withdrawal symptoms of abinones because of its alpha 2 agonist effect, but it does not relieve anxiety and psychological craving and high relapse problems. Withdrawal from heroin and methadone is more effective than withdrawal from morphine. It can also be used as an adjunctive treatment for obsessive-compulsive disorder, panic disorder, and tic-tac-toe syndrome. It is easily absorbed orally, Tmax is 2~4h, T1/2 is 7~13h, and the effect can be maintained for 6h. It can easily pass the blood-brain barrier, and 50% of the original drug and 20% of the bound metabolites are excreted from urine. Treatment of hypertension 0.15-0.3mg/d, divided into 2-3 doses. For the treatment of tic disorder, 0.0375-0.075mg/d is commonly used, divided into 1 to 2 oral doses, and the total amount can be gradually increased, not exceeding 0.45mg/d.
  Adverse reactions include drowsiness, dizziness, irritability, dry mouth, constipation, dry eyes and nasal mucosa. Occasionally, upright hypotension and tachycardia are seen. Withdrawal reactions may occur with long-term dosing. Not to be used with beta-blockers.
  3
  Benzodiazepine Flumazenil, trade name Anexate
  0.5mg/5ml
  Benzodiazepine antagonist. It can be used in anesthesia to promote awakening and drug poisoning resuscitation (restoration of natural breathing and withdrawal of tracheal intubation). T1/2=53min, the main metabolite is inactive benzodiazepine carboxylic acid, which is excreted via the kidney. Concomitant administration of benzodiazepines has no effect on the pharmacokinetics of Enzycare. For anesthesia, 0.2mg for the first time within 15s, if not awake after 60s, 0.1mg can be added, and then repeated every 60s until 1mg. the usual dose is 0.3-0.6mg. for poisoning, 0.3mg for the first time, if not awake after 60s, it can be repeated until awake or the total amount reaches 2mg. if drowsy again, 0.1-0.4mg/h.
  Side effects are nausea, vomiting, anxiety, palpitations, and fear, which generally do not require special treatment. Safe dose is 100mg or less at a time. When benzodiazepine dependent patients use may have withdrawal reaction, can intravenous push valium 5mg. benzodiazepines and cyclic antidepressants mixed poisoning, the toxicity of antidepressants will be overridden by the protective effect of benzodiazepines, in the presence of severe poisoning due to autonomic or cardiovascular symptoms of tricyclic/tetracyclic antidepressants, Ativan should not be used to reverse the effects of benzodiazepines.
  4
  Piracetam, alias amidopyrone, brain rejuvenation
  0.4*100
  Anti-hypoxic puzzle drug, can activate and protect neurons, improve various types of brain hypoxia and physical and chemical factors caused by brain damage, promote the brain to use phospholipids, amino acids, glucose and store energy. Improves microcirculation and red blood cell flexibility, inhibits platelet agglutination, etc. It is used for cerebral arteriosclerosis and cerebrovascular accident-induced memory and thinking loss, and also has an educational effect on mentally retarded children and mild to moderate Alzheimer’s disease. It is easily absorbed orally, with Tmax of 30-40 min and T1/2 of 4-6 h. It can pass the blood-brain and placental barriers and does not undergo degradation and biotransformation in the body. 94-98% of the original drug is excreted in the urine at 26-30 h of administration. Oral 0.4~0.8g/dose, 2~3 times/d.
  Adverse effects are mild.
  5
  Dihydroergotoxine, trade name Hydergine
  1mg*50
  Alters cerebral neurotransmission with excitatory effects on dopamine and 5-HT receptors and blocking effects on alpha receptors. Improves impaired cerebral metabolic function and shortens cerebral circulation time, causing changes in electroencephalographic activity. Tmax is 0.5~1.5h, bioavailability is 5~12% due to first pass effect, excreted by bile and feces, little need to reduce the dose in patients with renal dysfunction. Take 1 to 2 mg/d orally, 3 to 6 mg/d before meals.
  Occasional nasal congestion, transient nausea and gastric distress may occur and can usually be prevented by taking with food. Side effects generally do not require special treatment, and the dose can be adjusted if necessary. It should be used with caution in case of severe bradycardia.
  6
  Huperizinia strobilurum, trade name Huperzine Haberin
  50μg*24
  Reversible cholinesterase inhibitor with selective inhibition of true cholinesterase, easily crosses the blood-brain barrier, and has the effect of promoting memory reproduction and enhancing memory retention. Used with benign memory disorders to improve patients’ ability to point to memory, associative learning, image recall, meaningless graphic recollection and portrait recall. It also has an ameliorative effect on memory impairment caused by dementia and organic brain lesions. No accurate information on human pharmacokinetics is available. It is rapidly absorbed and distributed in animals, with a half distribution period of 9.8 min, and excreted mainly through the kidneys, with a slow excretion rate of 247.5 min.
  Adverse reactions are generally insignificant. Excessive doses may cause dizziness, nausea, gastrointestinal discomfort, malaise and other reactions, which can generally disappear on their own, and can be relieved or disappeared by dose reduction or discontinuation. Use with caution in patients with bradycardia and bronchial asthma.
  7
  Donepezil trade name Aricept
  5mg*30
  A specific reversible cholinesterase inhibitor for the treatment of mild or moderate AD. Tmax is 3-4h, T1/2 is about 70h, and steady state is reached in 3 weeks. Excreted as a prototype or metabolized by P450 enzymes, the metabolites are bound to glucuronide and excreted mainly via urine. Elimination is unaffected in renal function and mild to moderate hepatic insufficiency. Take at night at bedtime, initially 5 mg/d for at least 1 month to evaluate efficacy and achieve steady-state concentrations. It may be increased to 10mg/night. The efficacy gradually decreases after discontinuation of treatment, with no rebound on discontinuation.
  Adverse reactions are mild and mostly transient, mainly diarrhea and muscle cramps (incidence ≥ 5%), as well as malaise, nausea, vomiting, insomnia, and dizziness (incidence ≥ 5%). Caution should be exercised in patients with a history of asthma, obstructive pulmonary disease, “sick sinus syndrome” or other supraventricular cardiac conduction disorders. No adverse reactions related to drug interactions have been observed in combination with SSRIs, psychostimulants, or antiparkinsonian drugs. Overdose can cause cholinergic crisis. Atropine can be used on the basis of supportive therapy, with 1.0-2.0 mg given intravenously for the first time, and later administered according to clinical manifestations.