stimulants

The effects of stimulants, sources, etc.

1. Central nervous system stimulants A general expose.

2. Introduction to stimulants All stimulants cause an increase in general behavioural activity when taken short- term(one/two weeks), stimulants cause state of euphoria, optimism and general feelings of well-being. Initial feeling of anorexia are frequent. These responses indicate the involvement of the Hypothalamus. The dopamine transmitter system is primarily involved in many of its effects.

3. Stimulants what are they? DEFINITION : Psychoactive drugs that induce temporary improvement in either mental or physical functions or both. Effects include; alertness, wakefulness and locomotion. Stimulants are widely used as prescription medicines as well as without prescription(illicitly). Examples of Prescribed Stimulants; Amphetamines, Ephedrine, Caffeine, Nicotine etc. Examples of Illicit Stimulants; Cocaine, Crack Cocaine, Methamphetamine

4. Mechanism of action of stimulants 1. Block neurotransmitters reuptake   (Most reuptake inhibitors affect either NE or 5-HT(Serotonin) : Cocaine 2. Promote neurotransmitters release : Amphetamine 3. Block Metabolism - MAO inhibitors (monoamine oxidase):ex. Phenelzine 4. Antagonize the effect of inhibitory neurotransmitter: Picrotoxin & Strychnine

5. sources They are mostly obtained from Plant Sources; Cocaine ( Erythroxylum coca) Caffeine( Thea sinesis) Ephedrine (Ephedra sinica) Nicotine (Nicotiana tobaccum) Strychnine (Strychnox nux-vomica) Tea (Thea sinensis) Coffee ( Coffea arabica ) Theophylline / Theobromine (Theobroma cacao)

6. general indications of stimulants To counteract lethargy and fatigue throughout the day while at work or while doing other activities. To reduce sleepiness and to treat narcolepsy. To decrease appetite and promote weight loss and to treat obesity . The CNS stimulants are used to treat conditions characterized by lack of adrenergic stimulation, including narcolepsy (relatively rare sleep disorder) and neonatal apnea . They are also used, that is, (Ritalin, Dexedrine) for their paradoxical effect in attention – deficit hyperactivity disorder (ADHD). The benzphetamine , Sibutramine and the anorexiants are also used for appetite reduction in severe obesity. Because of their ability to improve mood and self-confidence, doctors prescribe stimulants in combination with anti-depressants to treat depression. Stimulants relax the bronchial muscles almost all asthma medications contain stimulants. Stimulants are also effective in treating cognitive disturbances in HIV patients and in cancer patients going through cranial irradiation.

7. GENERAL INDICATIONS Caffeine is often added to painkillers in order to make them more effective. Stimulants were also found to aid in smoking cessation (bupropion and nicotine), reduce sleepiness and to keep the person awake when necessary as well as to treat narcolepsy. In cases they are used to promote weight loss, as well as to treat obesity. In the late 1880s cocaine was used as remedy for morphine addiction suffered by many Civil War soldiers. Doctors used to numb the eye during surgery as it restricted bleeding because it tightened up the blood vessels. Later, in 1914 was added to the controlled list of drugs after its side and adverse effects had become well documented.

8. SIDE AND ADVERSE EFFECTS Stimulants have a number of common side effects; these include stomach upset, headache and increased blood pressure. Other adverse effects are insomnia, irritability, weakness, dizziness, tremor, hyperactive reflex. Adverse effects of stimulants on the gastrointestinal tract include anorexia, nausea, vomiting, abdominal cramps and diarrhoea. Stimulants also produce increased heart rate , increased blood pressure, heart failure and arousal .

9. Medical and Non- medical uses of stimulants Elevate Mood, Increase Motor Activity, Increase Alertness, Decrease need for Sleep, In case of overdose lead to convulsion and death. All stimulant drugs cause an increase in general behavioral activity. When taken short-term (one or two weeks), stimulant drugs cause states of euphoria, optimism, and general feelings of well-being. Initial feelings of anorexia are frequent, a quality that leads to their use/abuse in weight loss products. Insomnia is also frequent. These responses indicate that the part of the brain which controls these functions, the hypothalamus, is strongly affected by these drugs and that the dopamine transmitter system is primarily involved in many of these effects. Other effects are: • decreased feelings of depression, increased thoughts and associations, increased talkativeness, increased blood pressure, anxiety, irritability, decreased fatigue

10. classifications Analeptic Stimulants : these are restorative or stimulative medicines, used to overcome depression. E.g. Strychnine. Psychomotor Stimulants ; these are psychotropic medications that stimulate the CNS by boosting the release of certain chemicals. E.g. Amphetamine, Methamphetamine, Ephedrine, Methylphenidate. Methylxanthines ; these are E.g. Cocaine, Caffeine, Theophylline, Theobromine.

11. Analeptic stimulants These are central nervous system stimulants used to treat ADHD (Attention Deficit Hyperactivity Disorder ) and Respiratory Depression . They are also used as convulsants . They act as Serotonin Receptor Agonists or Potassium Channel blockers. E.g. Doxapram. Analeptics have been used throughout history for two main purposes ; helping patients recover from Anaesthesia more efficiently and the management of respiratory distress and apnoea. FORMS: They generally occur in tablet formulation.

12. STRYCHININE MOA: Competitive antagonist of the glycin receptors.   After injecting the mice with Strychinine you well notice:   - Tonic convulsion characterized by : 1. Symmetric 2. Reflex in origin 3. Continuous 4. Uncoordinated.

13. Side effects of analeptics; Sweating Nausea Vomiting Urinary retention and muscle spasticity Diarrhoea

14. Psychomotor stimulants; AMPHETAMINES Mechanism of action;    Block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extra neuronal space.   Clinical use: 1. Narcolepsy,. 2. Attention-deficit hyperactivity disorder AFTER ADMINISTRATION: Hair Erection, Licking, Sniffing are major side effects

15. amphetamines common names;

16. TYPES OF AMPHETAMINES Designer drugs: are a product of amphetamine and methamphetamine that have prominent psychedelic effects in addition to their CNS stimulatory action. Some designer drugs are… Meth cathinone (combination of methamphetamine and cocaine) Methylenedioxy -n- methylamphetamine (MDMA, Ecstasy)(Stimulant and Hallucinogen) Methylenedioxyamphetamine Detroamphetamine : Used for ADHD and narcolepsy Levoamphetamine : A psychostimulant used to increase alertness

17. Adverse effects : Cardiovascular: Hypertension (7% to 22%, pediatric ) Endocrine metabolic: Weight loss (4% to 9%, pediatric; 11%, adults ) Gastrointestinal: Abdominal pain (11% to 14%, pediatrics ), Loss of appetite (22% to 36%), Xerostomia (35% ) Neurologic: Headache (26% ), Insomnia (12% to 17%), pediatric; (27%, adults ) Psychiatric: Feeling nervous (6% )  

18. Forms

19. Amphetamine effects

20. Cocaine MECHANISM OF ACTION; Binding with adenosine (“purine”) receptors in brain (endogen ligand of these receptors – adenosine - decreases processes of excitation in CNS) Inhibiting of phosphodiesterase, which leads to accumulation of cAMP and stimulation of many physiological processes and metabolism

21. Pharmacological effects ; CNS -behavioral effects result from powerful stimulation of cortex and brain stem. Cocaine acutely increases mental awareness and produces a feeling of wellbeing and euphoria similar to that produced by amphetamine. Like amphetamine, cocaine can produce hallucinations and delusions of paranoia or grandiosity. Cocaine increases motor activity, and at high doses, it causes tremors and convulsions, followed by respiratory and vasomotor depression.

22. Pharmacological effects of cocaine Enhanced activity of dopamine, noradrenaline, adrenaline and serotonin transmitters Blocks the reuptake and inactivation of these elements following their release from neurons CNS Effects Creates increased strength, energy, and performance Increases euphoria, self-confidence, well-being, and sociability Cardiovascular System Effects Increases the levels of adrenaline, increases heart rate, raises blood pressure Local Anesthetic Effects Reduces bleeding Topical numbing effects

23. cocaine

24. forms

25. Mode of administration

26. Crack cocaine Already processed cocaine and making it pure again is crack cocaine Could contain as much as 90% pure cocaine Inexpensive Typically smoked in a glass water pipe A rush or high happens within 8 to 10 seconds The high can last about 3 to 5 minutes “Crash” occurs for 10 to 40 minutes Extreme state of depression

27. methylxanthines 1.Theophylline (found in tea): long-acting, prescribed for night-time asthma 2.Theobromine: found in cocoa. 3.Caffeine: (short-acting) the most widely consumed found in coffee (200 mg/cup), carbonated soft drinks (60 mg/can), cocoa and chocolate

28. Pharmacologic actions of caffeine Vessels: Stimulation of vasomotor center ;contraction of vessels, increasing of BP, Peripheral myotropic spasmolytic action – dilation of vessels, decreasing of BP Heart : Central action (increasing of n. vagus tone) – bradycardia, Peripheral action (direct influence on heart) – tachycardia, possible extrasystolia Diuretic effect : It has a mild diuretic action that increases urinary output of sodium, chloride and potassium Gastric mucosa : Since all methylxantines stimulate secretion of hydrochloric acid ( HCl ) from the gastric mucosa, individuals with peptic ulcers should avoid beverages containing methylxantines

29. Adverse effects If administered regularly – psychological addiction – theism, which is accompanied by development of abstinent syndrome (headache, retardness , fatigue, somnolence, depression) Insomnia, anxiety, agitation Acute poisoning in case of overdosing (lethal dose – 10g for caffeine – about 100 cups)

30. Adverse effects; Increased happiness and excitement Talk, move, and think quickly, alertness, wakefulness, restlessness, Heart beats faster, Nervousness and anxiety Mood swings Aggressiveness Paranoia, Twitching and shaking of the body Increased Blood Pressure, Could lead to heart attack or stroke Suppressed appetite, Possible weight loss

31. ADVERSE EFFECTS Anxiety reaction that includes: hypertension, tachycardia, sweating, and paranoia. Because of the irritability, many users take cocaine with alcohol. A product of cocaine metabolites and ethanol is cocaethylene , which is also psychoactive and cause cardiotoxicity.

32. effects a. CNS: decrease in fatigue, increased alertness: 100-200 mg caffeine in 1 or 2 cups of coffees Spinal cord stimulation: 2-5 g (very high dose) Tolerance can rapidly develop Withdrawal symptoms: feeling of fatigue & sedation. b. CVS: at high dose of caffeine + ve inotropic and chronotropic effects on the heart, ↑COP c. Diuretic action: mild ↑ urinary output of Na+, Cl-and K+ d. Gastric mucosa: all methylxanthines stimulate secretion of HCl e. Respiratory smooth muscle: bronchodilator, Rx asthma replaced by β- agonists, corticosteroids.

33. Caffeine and caffeine like products (xanthines) CNS Effects 100-200 mg/day - Alertness, arousal, and reduces tiredness 300+ mg/day – Insomnia, increased tension, anxiety, and muscle twitches 500+ mg/day – panic sensations, chills, nausea, and clumsiness Extreme doses/day – May result in seizures, respiratory failure, and even death Cardiovascular and Respiratory Effects 500+ mg leads to increased heart activity Can help with asthma-related respiratory problems

34. Adverse effects Moderate doses: insomnia, anxiety, agitation High doses: emesis, convulsion Lethal dose (10 gm of caffeine): cardiac arrhythmia Suddenly stop: lethargy, irritability, headache

35. Mode of administration

36. nicotine Nicotine is the active ingredient in tobacco. Used in smoking cessation therapy, Actions of Nicotine: Low dose: ganglionic depolarization High dose: ganglionic blockade

37. effects CNS: 1.Low dose: euphoria, arousal, relaxation, improves attention, learning, problem solving and reaction time. 2.High dose: CNS paralysis, severe hypotension (medullary paralysis) II. Peripheraleffects : Stimulation of sympathetic ganglia and adrenal medulla→↑ BP and HR (harmful in HTN patients), Stimulation of parasympathetic ganglia→↑ motor activity of the bowel At higher doses, BP falls & activating ceases in both GIT and bladder. The acute lethal dose is 60 mg. Adverse effects: CNS: irritability and tremors, Intestinal cramps, diarrhea, ↑HR & BP

38. Withdrawal symptoms of cns stimulants

39. remedy The first step of treating an addiction is detoxification (the process of letting the body remove drugs in it). During detox, doctors manage the physical part of the addiction by getting the stimulants out of the person’s system. Detox typically lasts up to a week but could last longer depending on the severity of the addiction. Also, the type of stimulant used affects how long it takes to detox; for example, people addicted to cocaine tend to have a short time to detox than people addicted to prescription stimulants like Adderall. Some studies have been able to come up with certain drugs that may reduce cravings and lead to a successful recovery. Examples of such drugs are Prozac which is prescribed for mood disorders like depression and obsessive compulsive disorder and also Naltrexone, which has also shown potential in treating prescription stimulant-depression.

40. remedy Psychotherapy and counselling may also be used in alleviating problems in cases. Psychotherapy is a general term for treating mental health problems by talking with a psychiatrist, psychologist or other mental health provider. During psychotherapy, you learn about your condition and your moods, feelings, thoughts and behaviours. Reduction of dose of stimulants using devices such as the electronic cigarette and chewing gums, is also another alternate remedy. In the cases of remedy for smoking habits, cigarette, containing nicotine, is substituted with electronic cigarettes which can be regulated to stop the habit in entirety. Medicated chewing gums may also be recommended instead of the electronic cigarette depending on the intensity of the addiction.

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