Psychostimulants ,Adaptogens, Analeptics, Antidepressants and Nootropic Drugs
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The document details various classes of drugs, including psychostimulants, adaptogens, analeptics, antidepressants, and nootropics, and their mechanisms of action. It describes the pharmacological effects, clinical uses, and potential adverse effects of specific medications such as caffeine, amphetamines, tricyclic antidepressants, and selective serotonin reuptake inhibitors. Additionally, the document discusses the impact on mental and physical capacities and addresses specific medical conditions that these drugs are used to treat.
![Clinical Uses of Analeptics
Acute Respiratory Failure:
Aggravation of COPD [Chronic Obstructive Pulmonary
Diseases] with sleepiness, inability to cough out
Respiratory depression during Infectious Diseases,
Shock, Syncopal conditions
Asphyxia (Respiratory Arrest) of Newborns and
during surgical operations
Poisons with Hypnotic drugs, Opioid Analgesics,
General Anesthetics
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Psychostimulants ,Adaptogens, Analeptics, Antidepressants and Nootropic Drugs
- 2. Psychostimulants (Psychomotor Stimulants) 1. Methylxanthines: Caffeine (Coffeinum-natrii benzoas ) tab. 0.1 g; amp. 10% and 20% - 1 ml) 2. Phenylalkyl amines: Phenamine (Amphetamine) 3. Phenylalkyl sydnonimines: Sydnocarb (tab. 0.005 and 0.01 g) 4. Piperidine compounds: Meridil (tab. 10 mg) 2
- 3. Mechanisms of Action of Caffeine 1). Blockade of Phosphodiesterase => cAMP and cGMP 2) Blockade of ADENOSINE Receptors ADENOSINE – an Inhibitory Transmitter of the CNS inhibits Adenyl Cyclase activity, causing Contraction of Airway Smooth Muscle 3
- 4. ATP Adenyl Cyclase cAMP or ─────── or ─── GTP Guanyl Cyclase cGMP cAMP 5-AMP or ──────── cGMP Phosphodiesterase 5-GMP Inhibited by Methylxanthines 4
- 5. Pharmacological Effects of Caffeine : Stimulation of Medullary, Vagal, Respiratory and Vasomotor centers Cardiac Output and Cardiac Work (+) Inotropic and (+) Chronotropic Effects Improvement of : ●Coronary, Cerebral and Renal Circulation, ● Eye Ground Blood Circulation ● Acuity of Vision and Color Vision Smooth muscles relaxation, most prominent effect – on Bronchi, esp. in asthmatics Clinical Uses: CNS depression, Neonatal Apnea, Hypotension. 5
- 6. Phenamine (Amphetamine)- a central sympathomimetic. It was synthesized in the late 1920s and has a large number of analogs including Dexamphetamine, Methamphetamine, Methylene-dioxymeth-amphetamine (MDMA, or "Ecstasy"). Phenamine is chemically a phenylalkylamine, i.e. its structure is similar to noradrenaline and adrenaline. It has the same pharmacological profile as Ephedrine; orally active with long duration (4-6 hours). Mechanism of action. Phenamine acts primarily by releasing noradrenaline and dopamine in the brain, inhibits catecholamines reuptake, MAO activity and increases receptors sensitivity to catecholamines. Clinical uses: attention deficit disorder, narcolepsy (an uncontrollable desire for sleep). 6
- 7. Sydnocarb (Mesocarb) – chemically and pharmacologically similar to phenamine but does not cause drug dependence, hypnosis, less influences on peripheral adrenoreceptors. Sympathomimetic and cardiovascular actions are insignificant. Mechanism of action: Catecholamines Reuptake MAO activity Receptors Sensitivity to Catecholamines Clinical uses: Neurotic disorders, Attention deficit hyperkinetic disorder, Narcolepsy, Asthenia, Apathy, Excessive day time sleepiness, Decreased working capacity. Adverse effects: anorexia, insomnia, abdominal discomfort and bowel upset, AP increase. 7
- 8. ADAPTOGENS 1. Plant origin – Powders, T-res and Extracts from roots or fruit of: Ginseng, Eleutherococcus, Rhodiola, Schizandra, Aralia 2. Animal origin –Extracts from antlers of the young Siberian males of a deer – Pantocrin, Rantatrin Mechanism of Action: 1). Activation of RNA and Protein synthesis 2). Biochemical Disorders in Stress Reactions 3). Normalization of Pituitary-Adrenal and Immune System functions 8
- 9. Pharmacodynamics Physical and Mental Capacity Fatigue, Appetite Disorders Tolerance to Harmful Influences, High to, Cooling, Intoxications; Ionizing Radiation Specific and Non- Specific Immunity Improvement: Blood Circulation, Breathing, Vision and Hearing, Cardio-Protector and Hepato-Protector effect Ginseng Eleutherococcus 9
- 10. Clinical Uses: Physical Overwork Physical and Mental Overfatigue Asthenic Syndrome State after Infection and Somatic Diseases Ionizing Radiation Influence Adverse effect: Overexcitement of Nervous and Cardio-Vascular system, Arterial Hypertension, Hyperglycemia Rhodiola 10
- 11. Classification of ANALEPTICS 1. With prevalent action upon the BRAIN CORTEX Caffeine Caffeine-Natrium Benzoate 2. With prevalent action upon the MEDULLA OBLONGATA: Bemegride– amp. 0.5%-10 ml Etimizol – amp. 1.5%-3 ml Cordiamin – amp. 1 ml, vial 15 and 30 ml Sulfocamphocaine – amp. 10%-2 ml 3. With prevalent action on the SPINAL CORD: Strychnine Nitrate Strength According to Analeptic Activity: Bemegride – Cordiamin - Sulfocamphocaine - Etimizol 11
- 12. Clinical Uses of Analeptics Acute Respiratory Failure: Aggravation of COPD [Chronic Obstructive Pulmonary Diseases] with sleepiness, inability to cough out Respiratory depression during Infectious Diseases, Shock, Syncopal conditions Asphyxia (Respiratory Arrest) of Newborns and during surgical operations Poisons with Hypnotic drugs, Opioid Analgesics, General Anesthetics 12
- 13. Etimizol amp. 1.5% - 3 ml, tab. 0.1 g – an analeptic of direct action 1. Direct excitement of the Respiratory Center 2. ACTH production => Glucocorticoids’ level in blood - is used as Anti-inflammatory and Antiallergic agent to treat Arthritis, Polyarthritis, Asthma 3. Acceleration and Deepening of Respiration 4. HR, BP. Clinical uses: Respiratory failure in Shock; Collapse, Asphyxia; Respiratory Depression in Infectious Diseases; Prophylaxis of Lung Atelectasis and Pneumonia, Arthritis, Polyarthritis, Asthma 13
- 14. Cordiamin (Niketamide) – amp. 1 ml, vial 30 ml – an analeptic of mixed action direct exciting influence on Respiratory Center Stimulates N-Receptors of Carotid Sinus Acceleration and Deepening of Respiration HR, BP Clinical uses: Respiratory failure in Shock, Collapse, Asphyxia; Respiratory depression in Infectious diseases; Prophylaxis of lung atelectasis and pneumonia Adverse effects: clonic seizures, face hyperemia 14
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- 17. MAO A – NORADRENALINE and SEROTONIN, MAO B – DOPAMINE, PHENYLETHYLAMINE, TYRAMINE MAO A – NORADRENALINE and SEROTONIN, MAO B – DOPAMINE, PHENYLETHYLAMINE, TYRAMINE 17
- 18. Amitriptyline (tab. 0.01 and 0.025 g) – a Tricyclic Antidepressant. Inhibits reuptake of Noradrenaline and Serotonin in Nerve Terminals (Presynaptic Neurons) => => their Level in the synaptic cleft. More actively inhibits reuptake of Serotonin than Noradrenaline => SEDATION. Anxiolytic, Sedative and Psychomotor Dampening effects. Clinical uses: Depression, Anorexia, Bulimia. 18
- 19. Adverse Effects of Tricyclic Antidepressants Antagonism at M-cholinoceptors Atropine-like effects: Tachycardia Inhibition of Exocrine Glands Xerostomia (dry mouth) Urinary retention Constipation Blurred vision Aggravation of Glaucoma and Epilepsy 19
- 20. Fluoxetine (Prozak – tab. 0.02 g) - a Selective Serotonin-Reuptake Inhibitor (SSRI) – specifically inhibits SEROTONIN reuptake Advantages include: Absence of cardiotoxicity Free of Anti-Cholinergic Effects, orthostatic hypotension Loss of appetite and Weight Reduction the ease of once-a-day dosing Clinical Uses: Depression, Bulimia nervosa, Obsessive-Compulsive disorder, Anorexia nervosa, Panic disorder, Premenstrual Syndrome Adverse Effects: Over arousal, Insomnia, Tremor, Anxiety, Akathisia (a state of Agitation, Distress, Restlessness and the Inability to sit still), sexual dysfunction, hot flashes, cough, flu-like syndrome 20
- 21. MAO Inhibitors: Nialamide, Moclobemide and SSRI : Fluoxetine et al. should not be co-administered due to the risk of Life Threatening "Serotonin Syndrome" as a result of excess SEROTONIN (5-HT): to, Muscle Rigidity, Myoclonus, Rapid Changes in Mental Status and Vital Signs Cardiovascular collapse Drugs require WASHOUT PERIODS of 6 weeks before administering the other. 21
- 22. Nootrop Drugs – activate learning, improve memory and intellectual activity I. ACTOPROTECTORS: 1. Activators of Brain Metabolism: Methyl Xanthines: Instenon Caffeine Aminophylline (Euphylline) Protein Hydrolyzates: Actovegin Cerebrolysin Solcoseryl 2. Cerebral Vasodilators: Nicergoline (Sermion) Vinpocetine 22
- 23. 3. Ca2+- Antagonists: Nimodipine, Cinnarizine 4. Antioxidants: Tocopherole acetatate (Vitamin E) 5. GABA and its derivatives: Aminalon (GABA) Oxybutyrate Sodium (GOBA) Pantogam, Phenibut, Picamilon II. Affecting Advantageously MEMORY: 1. Racetams - cyclic GABA derivatives: Piracetam (Nootropil) Aniracetam Oxiracetam 2. Pyridoxine (Vitamin B6) derivatives: Encephabol 23
- 24. Actovegin - amp. 4% 2 and 5 ml, vial 20%-250 ml, Dr. 0.2 g, is proved to be the Most Effective Nootrop. contains Deproteinized Hemoderivate from plasma of the Calf blood with Low-molecular Peptides, Amino Acids, Nucleosides, Lipids, Electrolytes and Microelements. After 60-90 min IV infusion of 20% 250 ml: Cardiac Index by 25% Stroke Index by 30% O2 Content in Arterial Blood by 13% HR does not change Intensity and Efficiency of Aerobic Processes Energy and Contractibility of Muscles Prevents accumulation of LACTATE in them 24
- 25. Instenon – 1 ampoule with 2 ml contains: Methylxantine Ethophylline - 100 mg Analeptic Etamivan - 50 mg Vasodilator Hexobendin- 10 mg Cardiac Output Perfusion Pressure in the Vessels of the Edge Zone of Ischemia STIMULATES: the Respiratory and Vasomotor centers Centers of vegetative regulation Nuclei of the cranial nerves. Clinical uses: brain diseases of vascular and age-dependent nature, stroke, sequences of cerebrovascular insufficiency. 25
- 26. Cerebrolysin amp. 21.5% 1, 5 and 10 ml a peptidergic nootrop with neurotrophic action. 1 ml Є 215 mg of NEUROPEPTIDES from the Swine’s Cerebrum. Pharmacological action: nootrop, Metabolic regulation Neuroprotection Functional Neuromodulation Neurotrophic activity - analogous to natural Neuron Growth Factors 26
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- 29. Piracetam (amp. 20%-5 ml, tab. 0.4 g) - a derivative of GABA Mechanism of action: Improvement of metabolic and bioenergetic processes in neuron: Activation of synthesis of proteins and RNA Improvement of utilization of glucose Intensification of ATP synthesis Membrane-stabilizing action In large doses and at repeated introduction it is capable to strengthen GABA-ergic inhibitory processes in brain 29