Stimulants

Stimulants are used by the general public to increase alertness and energy, decrease fatigue, and promote mental focus. Stimulants have medical uses for individuals with ADHD and sleep Sleep Sleep is a reversible phase of diminished responsiveness, motor activity, and metabolism. This process is a complex and dynamic phenomenon, occurring in 4-5 cycles a night, and generally divided into non-rapid eye movement (NREM) sleep and REM sleep stages. Physiology of Sleep disorders, and are also used in combination with analgesics in pain management Pain Management Pain is defined as an unpleasant sensory and emotional experience associated with actual or potential tissue damage. Pain is a subjective experience. Acute pain lasts < 3 months and typically has a specific, identifiable cause. Pain Management. Stimulants are used in beverages and as over-the-counter medications, prescription medications, and drugs of abuse. Caffeine and nicotine are commonly used psychostimulants. Amphetamines are used in a clinical setting for specific indications, but are more often used illegally as drugs of abuse along with cocaine. Each agent has its idiosyncrasies with respect to effects, withdrawal, and overdose.

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Editorial responsibility: Stanley Oiseth, Lindsay Jones, Evelin Maza

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Caffeine

Overview

  • Mechanism of action: CNS stimulant
  • Chemistry: methylxanthine class
  • Most commonly consumed stimulant worldwide
  • Naturally occurring in several plants native to South America and East Asia, most notably in the coffee plant

Pharmacodynamics and pharmacokinetics

  • Mechanism of action:
    • Nonselective antagonist of adenosine → inability of adenosine to bind to its receptor → sensation of increased energy and alertness
    • Induces intracellular calcium release → stronger cardiac contractions
  • Absorption: GI tract
  • Distribution: peak plasma concentrations achieved between 30 minutes and 2 hours
  • Half-life: 5 hours
  • Metabolism: hepatic cytochrome P450 (CYP)1A2
  • Excretion: renal

Effects

  • Increased alertness, decreased fatigue
  • Increased metabolic rate
  • Anxiety
  • Vasoconstriction
  • Increased blood pressure
  • Mild diuretic

Clinical uses

  • Stimulant to promote wakefulness (Vivarin, NoDoz available over the counter (OTC))
  • Enhances analgesic effect in combination medications and used in both OTC and prescription medications:
    • Acetaminophen Acetaminophen Acetaminophen is an over-the-counter nonopioid analgesic and antipyretic medication and the most commonly used analgesic worldwide. Despite the widespread use of acetaminophen, its mechanism of action is not entirely understood. Acetaminophen/aspirin/caffeine
    • Hydrocodone/acetaminophen/caffeine
    • Acetaminophen Acetaminophen Acetaminophen is an over-the-counter nonopioid analgesic and antipyretic medication and the most commonly used analgesic worldwide. Despite the widespread use of acetaminophen, its mechanism of action is not entirely understood. Acetaminophen/caffeine/pyrilamine (OTC Midol)
    • Butalbital/acetaminophen//caffeine/codeine
    • Orphenadrine/aspirin/caffeine
  • Respiratory stimulant: used for apnea of prematurity in infants
  • Migraine Migraine Migraine headache is a primary headache disorder and is among the most prevalent disorders in the world. Migraine is characterized by episodic, moderate to severe headaches that may be associated with increased sensitivity to light and sound, as well as nausea and/or vomiting. Migraine Headache and cluster headache (in prescription Cafergot and OTC Excedrin Migraine Migraine Migraine headache is a primary headache disorder and is among the most prevalent disorders in the world. Migraine is characterized by episodic, moderate to severe headaches that may be associated with increased sensitivity to light and sound, as well as nausea and/or vomiting. Migraine Headache)
  • Postdural puncture headache
  • Mild diuretic (OTC Diurex)
  • Used topically/transdermally in cosmetic preparations

Adverse effects and contraindications

  • Adverse effects:
    • Tachyarrhythmias
    • Anxiety
    • Hypertension Hypertension Hypertension, or high blood pressure, is a common disease that manifests as elevated systemic arterial pressures. Hypertension is most often asymptomatic and is found incidentally as part of a routine physical examination or during triage for an unrelated medical encounter. Hypertension
    • Rash, epidermal thinning, xeroderma
    • Gastritis Gastritis Gastritis refers to inflammation of the gastric mucosa. Gastritis may occur suddenly (acute gastritis) or slowly over time (chronic gastritis). Gastritis may be asymptomatic or with symptoms, including burning abdominal pain (which either worsens or improves with eating), dyspepsia, nausea, and vomiting. Gastritis/GI hemorrhage
    • Tolerance and dependence
    • Seizures Seizures A seizure is abnormal electrical activity of the neurons in the cerebral cortex that can manifest in numerous ways depending on the region of the brain affected. Seizures consist of a sudden imbalance that occurs between the excitatory and inhibitory signals in cortical neurons, creating a net excitation. The 2 major classes of seizures are focal and generalized. Seizures in high doses
  • Contraindications:
    • Vascular disease where vasoconstriction may cause occlusion
    • Caution with:
      • Hypertension Hypertension Hypertension, or high blood pressure, is a common disease that manifests as elevated systemic arterial pressures. Hypertension is most often asymptomatic and is found incidentally as part of a routine physical examination or during triage for an unrelated medical encounter. Hypertension
      • Arrhythmias
      • Hyperthyroidism Hyperthyroidism Thyrotoxicosis refers to the classic physiologic manifestations of excess thyroid hormones and is not synonymous with hyperthyroidism, which is caused by sustained overproduction and release of T3 and/or T4. Graves' disease is the most common cause of primary hyperthyroidism, followed by toxic multinodular goiter and toxic adenoma. Thyrotoxicosis and Hyperthyroidism
      • Peptic ulcer Peptic ulcer Peptic ulcer disease (PUD) refers to the full-thickness ulcerations of duodenal or gastric mucosa. The ulcerations form when exposure to acid and digestive enzymes overcomes mucosal defense mechanisms. The most common etiologies include Helicobacter pylori (H. pylori) infection and prolonged use of non-steroidal anti-inflammatory drugs (NSAIDs). Peptic Ulcer Disease/GI bleed
      • Anxiety disorders

Drug-drug interactions

  • Isocarboxazid (monoamine oxidase inhibitor (MAOI)) → hypertension
  • May decrease lithium levels
  • May increase tizanidine levels → risk of hypotension Hypotension Hypotension is defined as low blood pressure, specifically < 90/60 mm Hg, and is most commonly a physiologic response. Hypotension may be mild, serious, or life threatening, depending on the cause. Hypotension and bradycardia
  • Methotrexate → decreases efficacy due to adenosine receptor antagonism
  • Theophylline (also a methylxanthine) → risk of arrhythmias, seizures

Withdrawal syndrome

  • Clinical presentation:
    • Headache
    • Lethargy
    • Irritability
  • Management: gradual reduction in dosage/use

Overdose and toxicity

  • Clinical presentation:
    • Hypertension Hypertension Hypertension, or high blood pressure, is a common disease that manifests as elevated systemic arterial pressures. Hypertension is most often asymptomatic and is found incidentally as part of a routine physical examination or during triage for an unrelated medical encounter. Hypertension, followed by hypotension Hypotension Hypotension is defined as low blood pressure, specifically < 90/60 mm Hg, and is most commonly a physiologic response. Hypotension may be mild, serious, or life threatening, depending on the cause. Hypotension
    • Mydriasis
    • CNS stimulation:
      • Tremors
      • Insomnia Insomnia Insomnia is a sleep disorder characterized by difficulty in the initiation, maintenance, and consolidation of sleep, leading to impairment of function. Patients may exhibit symptoms such as difficulty falling asleep, disrupted sleep, trouble going back to sleep, early awakenings, and feeling tired upon waking. Insomnia
      • Anxiety
    • Hyperreflexia
    • Altered mental status, agitation, delusional thoughts, hallucinations, and seizures
  • Management:
    • Supportive care
    • Beta-blockers for tachycardia
    • Procainamide or amiodarone for tachyarrhythmias
    • Activated charcoal may be useful if ingestion was recent (overdose of pills).
Main symptoms of caffeine overdose

Main symptoms of caffeine overdose

Image: “Main symptoms of caffeine overdose” by Mikael Häggström. License: Public Domain

Nicotine

Overview

  • Naturally occurring; tobacco plant native to the Americas
  • Modes of use:
    • Cigarette smoking
    • Tobacco chewing
    • Vaping/inhaling
  • Chemistry:
    • Natural alkaloid
    • 3-(1-Methyl-2-pyrrolidinyl)pyridine

Pharmacodynamics and pharmacokinetics

  • Mechanism of action:
    • Stimulates the nicotinic cholinergic receptors in the brain, autonomic ganglia, and neuromuscular junctions → cortical stimulation → sensation of increased energy 
    • Limbic system Limbic system The limbic system is a neuronal network that mediates emotion and motivation, while also playing a role in learning and memory. The extended neural network is vital to numerous basic psychological functions and plays an invaluable role in processing and responding to environmental stimuli. Limbic System → rewarding effect
  • Absorption:
    • Pulmonary (tobacco smoke)
    • Oral mucosa (chewing tobacco)
    • Prescription forms used for smoking-cessation therapy:
      • Transdermal
      • Intranasal
  • Half-life:
    • 1–2 hours when inhaled
    • 4 hours when administered transdermally
  • Distribution: Peak plasma concentration:
    • 15 minutes when inhaled
    • 2–8 hours when administered transdermally
  • Metabolism: hepatic (most predominantly), renal, and pulmonary
  • Excretion: renal

Effects

  • Increased alertness
  • Increased metabolic rate
  • Anxiety
  • Vasoconstriction
  • Increased blood pressure

Clinical uses

Smoking-cessation therapy (nicotine patch, gum, nasal spray, or inhaler)

Adverse effects and contraindications

  • Adverse effects:
    • Tolerance and dependence: nicotine-use disorder
    • Cardiovascular:
      • Chest pain Chest Pain Chest pain is one of the most common and challenging complaints that may present in an inpatient and outpatient setting. The differential diagnosis of chest pain is large and includes cardiac, gastrointestinal, pulmonary, musculoskeletal, and psychiatric etiologies. Chest Pain
      • Hypertension Hypertension Hypertension, or high blood pressure, is a common disease that manifests as elevated systemic arterial pressures. Hypertension is most often asymptomatic and is found incidentally as part of a routine physical examination or during triage for an unrelated medical encounter. Hypertension
      • Palpitations
      • Tachycardia
    • GI:
      • Nausea
      • Constipation Constipation Constipation is common and may be due to a variety of causes. Constipation is generally defined as bowel movement frequency < 3 times per week. Patients who are constipated often strain to pass hard stools. The condition is classified as primary (also known as idiopathic or functional constipation) or secondary, and as acute or chronic. Constipation or diarrhea Diarrhea Diarrhea is defined as ≥ 3 watery or loose stools in a 24-hour period. There are a multitude of etiologies, which can be classified based on the underlying mechanism of disease. The duration of symptoms (acute or chronic) and characteristics of the stools (e.g., watery, bloody, steatorrheic, mucoid) can help guide further diagnostic evaluation. Diarrhea
    • Neurological:
      • Headache
      • Insomnia Insomnia Insomnia is a sleep disorder characterized by difficulty in the initiation, maintenance, and consolidation of sleep, leading to impairment of function. Patients may exhibit symptoms such as difficulty falling asleep, disrupted sleep, trouble going back to sleep, early awakenings, and feeling tired upon waking. Insomnia
  • Contraindications/cautions for prescription nicotine use:
    • Arrhythmia
    • Recent MI MI MI is ischemia and death of an area of myocardial tissue due to insufficient blood flow and oxygenation, usually from thrombus formation on a ruptured atherosclerotic plaque in the epicardial arteries. Clinical presentation is most commonly with chest pain, but women and patients with diabetes may have atypical symptoms. Myocardial Infarction within 2 weeks
    • Severe hepatic or renal disease
    • Angina
    • Hypertension Hypertension Hypertension, or high blood pressure, is a common disease that manifests as elevated systemic arterial pressures. Hypertension is most often asymptomatic and is found incidentally as part of a routine physical examination or during triage for an unrelated medical encounter. Hypertension

Drug-drug interactions

  • Bupropion: may increase the risk of hypertension even when used for smoking-cessation support
  • Dosage adjustments may be required when used with other CYP2A6 substrates.
  • Nicotine given for smoking-cessation support may decrease the effects of antidiabetic medications (glimepiride, glyburide, saxagliptin, rosiglitazone) → hyperglycemia
  • Other drugs may need similar dose adjustments after smoking cessation.
  • Varenicline: additive effect, may increase the risk of side effects

Withdrawal syndrome

  • Clinical presentation:
    • Irritability, impatience, hostility
    • Anxiety
    • Dysphoria or depressed mood
    • Difficulty in concentrating
    • Restlessness
    • Decreased HR
    • Increased appetite or weight gain
  • Management:
    • Bupropion: nicotinic antagonist; also used to treat depression
    • Varenicline:
      • Partial nicotinic acetylcholine receptor agonist
      • Reduces cravings
    • Alternative nicotine delivery methods: chewing gum, patch, nicotine inhaler

Overdose and toxicity

  • Nicotine toxicity can occur in users as well as in tobacco harvesters (“green tobacco sickness” due to transdermal absorption of nicotine from the surface of wet tobacco plants).
  • Clinical presentation:
    • Nausea/vomiting
    • Diarrhea
    • Dizziness
    • Dyspnea Dyspnea Dyspnea is the subjective sensation of breathing discomfort. Dyspnea is a normal manifestation of heavy physical or psychological exertion, but also may be caused by underlying conditions (both pulmonary and extrapulmonary). Dyspnea
    • Tachycardia
    • Seizures Seizures A seizure is abnormal electrical activity of the neurons in the cerebral cortex that can manifest in numerous ways depending on the region of the brain affected. Seizures consist of a sudden imbalance that occurs between the excitatory and inhibitory signals in cortical neurons, creating a net excitation. The 2 major classes of seizures are focal and generalized. Seizures
  • Treatment: supportive

Amphetamines

Overview

  • Group of synthetic sympathomimetic drugs Sympathomimetic drugs Sympathomimetic drugs, also known as adrenergic agonists, mimic the action of the stimulators (α, β, or dopamine receptors) of the sympathetic autonomic nervous system. Sympathomimetic drugs are classified based on the type of receptors the drugs act on (some agents act on several receptors but 1 is predominate). Sympathomimetic Drugs
  • Mostly illicit use; some medical indications
  • Chemistry: related to natural sympathomimetic amines
  • Derivatives used in a clinical setting:
    • Amphetamine sulfate
    • Dextroamphetamine
  • Variants available for illicit (street drug) use:
    • Methamphetamine
    • Methylenedioxymethamphetamine (MDMA), known as the street drug “ecstasy”
    • Produced in illegal laboratories

Pharmacodynamics and pharmacokinetics

  • Mechanism of action:
    • Promote the release of catecholamines (dopamine and norepinephrine) from their storage sites in the presynaptic nerve terminals
    • Less significant: blocking catecholamine reuptake by competitive inhibition
  • Absorption/routes of administration:
    • Clinical: oral/GI
    • Illicit: oral (pills), intranasal (snorting), inhalation (smoked), or IV use
  • Half-life: 9–14 hours
  • Metabolism: hepatic CYP2D6 substrate
  • Excretion:
    • Renal, largely unchanged
    • Needs dosage adjustment in advanced CKD CKD Chronic kidney disease (CKD) is kidney impairment that lasts for ≥ 3 months, implying that it is irreversible. Hypertension and diabetes are the most common causes; however, there are a multitude of other etiologies. In the early to moderate stages, CKD is usually asymptomatic and is primarily diagnosed by laboratory abnormalities. Chronic Kidney Disease
    • Depends on pH, higher excretion in acidic urine

Effects

  • CNS:
    • Increased alertness: used to treat narcolepsy Narcolepsy Narcolepsy is a neurological sleep disorder marked by daytime sleepiness and associated with cataplexy, hypnagogic hallucinations, and sleep paralysis. There are 2 types of narcolepsy: type 1 is associated with cataplexy and type 2 has no association with cataplexy. Narcolepsy
    • Increased focus and attention in individuals with ADHD
    • High risk of addiction Addiction Substance use disorders are a significant cause of morbidity and mortality, especially among adolescents and young adults. A substance-related and addictive disorder is the continued use of a substance despite harmful consequences; these include significant impairment to one's health or relationships or failure to fulfill major responsibilities at work, school, or home because of substance use. Substance-Related and Addictive Disorders (with both illicit and prescription use)
  • Cardiovascular:
    • Tachycardia
    • Vasoconstriction

Clinical uses

  • ADHD:
    • Amphetamine (generic; several brand name products)
    • Dextroamphetamine (Dexedrine)
    • Amphetamine/dextroamphetamine (Adderall)
    • Methamphetamine (Desoxyn)
    • Methylphenidate (Ritalin, Concerta): CNS stimulant but not an amphetamine derivative
  • Narcolepsy

Adverse effects and contraindications

  • Adverse effects (both illicit drugs and prescription):
    • Tolerance and dependence
    • General:
      • Anorexia, weight loss, or poor growth in childhood
      • Sleep disturbance, jitteriness, and emotional lability
      • Restlessness and irritability
    • Neurologic:
      • Insomnia Insomnia Insomnia is a sleep disorder characterized by difficulty in the initiation, maintenance, and consolidation of sleep, leading to impairment of function. Patients may exhibit symptoms such as difficulty falling asleep, disrupted sleep, trouble going back to sleep, early awakenings, and feeling tired upon waking. Insomnia
      • Headache
      • Tics Tics Tics and related diseases represent a set of neurobehavioral disorders of childhood that are characterized by sudden, repeated, nonrhythmic, stereotyped muscle movements sometimes accompanied by sounds or vocalizations. Tics and Tourette Syndrome
    • Psychiatric:
      • Anxiety/mania
      • Hallucinations/delusions
      • Diversion and misuse
    • Cardiovascular:
      • Tachycardia and dysrhythmias
      • Vasoconstriction
      • Hypertension Hypertension Hypertension, or high blood pressure, is a common disease that manifests as elevated systemic arterial pressures. Hypertension is most often asymptomatic and is found incidentally as part of a routine physical examination or during triage for an unrelated medical encounter. Hypertension
    • Skin Skin The skin, also referred to as the integumentary system, is the largest organ of the body. The skin is primarily composed of the epidermis (outer layer) and dermis (deep layer). The epidermis is primarily composed of keratinocytes that undergo rapid turnover, while the dermis contains dense layers of connective tissue. Structure and Function of the Skin:
      • Flushing
      • Delusional infestation → neurotic excoriations (with methamphetamine)
    • Other: priapism in adolescent boys
  • Chronic use (illicit drugs):
    • Psychosis (delusions, paranoia)
    • Necrotizing arteritis
    • Cerebral hemorrhage
    • CKD CKD Chronic kidney disease (CKD) is kidney impairment that lasts for ≥ 3 months, implying that it is irreversible. Hypertension and diabetes are the most common causes; however, there are a multitude of other etiologies. In the early to moderate stages, CKD is usually asymptomatic and is primarily diagnosed by laboratory abnormalities. Chronic Kidney Disease due to renal vessel vasculitis
  • Contraindications for clinical use:
    • History of drug abuse
    • Use of MAOI within 14 days
    • Motor tics or Tourette syndrome Tourette Syndrome Tics and related diseases represent a set of neurobehavioral disorders of childhood that are characterized by sudden, repeated, nonrhythmic, stereotyped muscle movements sometimes accompanied by sounds or vocalizations. Tourette syndrome is a severe form with symptoms lasting more than 1 year and involving both motor and vocal tics. Tics and Tourette Syndrome
    • Symptomatic cardiovascular disease/individuals with:
      • Structural heart defects
      • Cardiomyopathy Cardiomyopathy Cardiomyopathy refers to a group of myocardial diseases associated with structural changes of the heart muscles (myocardium) and impaired systolic and/or diastolic function in the absence of other heart disorders (coronary artery disease, hypertension, valvular disease, and congenital heart disease). Overview of Cardiomyopathies
      • Disturbances in heart rhythm
      • Advanced arteriosclerosis
    • Glaucoma Glaucoma Glaucoma is an optic neuropathy characterized by typical visual field defects and optic nerve atrophy seen as optic disc cupping on examination. The acute form of glaucoma is a medical emergency. Glaucoma is often, but not always, caused by increased intraocular pressure (IOP). Glaucoma
    • Hyperthyroidism Hyperthyroidism Thyrotoxicosis refers to the classic physiologic manifestations of excess thyroid hormones and is not synonymous with hyperthyroidism, which is caused by sustained overproduction and release of T3 and/or T4. Graves' disease is the most common cause of primary hyperthyroidism, followed by toxic multinodular goiter and toxic adenoma. Thyrotoxicosis and Hyperthyroidism
    • Moderate-to-severe hypertension
    • Psychiatric disorders:
      • Bipolar disorder Bipolar disorder Bipolar disorder is a highly recurrent psychiatric illness characterized by periods of manic/hypomanic features (distractibility, impulsivity, increased activity, decreased sleep, talkativeness, grandiosity, flight of ideas) with or without depressive symptoms. Bipolar Disorder
      • Schizophrenia Schizophrenia Schizophrenia is a chronic mental health disorder characterized by the presence of psychotic symptoms such as delusions or hallucinations. The signs and symptoms of schizophrenia are traditionally separated into 2 groups: positive (delusions, hallucinations, and disorganized speech or behavior) and negative (flat affect, avolition, anhedonia, poor attention, and alogia). Schizophrenia
      • Depression
      • Anxiety disorders

Drug-drug interactions

  • Coadministration of serotoninergic agents (e.g., fluoxetine) can cause serotonin syndrome Serotonin syndrome Serotonin syndrome is a life-threatening condition caused by large increases in serotonergic activity. This condition can be triggered by taking excessive doses of certain serotonergic medications or taking these medications in combination with other drugs that increase their activity. Serotonin Syndrome.
  • Coadministration of MAOIs can induce hypertensive crisis.

Withdrawal syndrome

  • Clinical presentation:
    • Acute phase (“the crash”): 1–2 days of dysphoria, drowsiness, insomnia
    • Subacute phase: mood offset → rebound depressive episode
  • Management:
    • Varying protocols include:
      • Benzodiazepines Benzodiazepines Benzodiazepines work on the gamma-aminobutyric acid type A (GABAA) receptor to produce inhibitory effects on the CNS. Benzodiazepines do not mimic GABA, the main inhibitory neurotransmitter in humans, but instead potentiate GABA activity. Benzodiazepines
      • Antidepressants
      • Antipsychotics
      • Behavioral therapy
    • Observe closely for suicidal ideation.

Cocaine

Overview

  • Naturally occurring compound found in the leaves of the coca plant native to South America
  • An illicit drug used worldwide; highly addictive/public health concern

Pharmacodynamics and pharmacokinetics

  • Mechanism of action:
    • Inhibition of dopamine, serotonin, and norepinephrine reuptake
    • Alpha-1, alpha-2, beta-1, and beta-2 adrenergic stimulation:
      • Alpha-adrenergic stimulation → vasoconstriction in both cardiac and peripheral vasculature
      • Beta-adrenergic stimulation → increased HR → tachyarrhythmia Tachyarrhythmia A tachyarrhythmia is a rapid heart rhythm, regular or irregular, with a rate > 100 beats/min. Tachyarrhythmia may or may not be accompanied by symptoms of hemodynamic change. Tachyarrhythmias
  • Absorption:
    • Medical use: topical
    • Street drug use: intranasal, IV, and inhaled (crack cocaine)
  • Distribution/time for effect:
    • Cocaine hydrochloride: 30 seconds
    • Crack cocaine: 8 seconds
  • Half-life: 0.5–1.5 hours
  • Excretion: renal

Effects

  • CNS stimulant
  • Local anesthetic

Clinical uses

  • Provides both topical anesthesia Anesthesia Anesthesiology is the field of medicine that focuses on interventions that bring a state of anesthesia upon an individual. General anesthesia is characterized by a reversible loss of consciousness along with analgesia, amnesia, and muscle relaxation. Anesthesiology: History and Basic Concepts and vasoconstriction
  • Useful in procedures involving highly vascularized mucosae in the nose Nose The nose is the human body's primary organ of smell and functions as part of the upper respiratory system. The nose may be best known for inhaling oxygen and exhaling carbon dioxide, but it also contributes to other important functions, such as tasting. The anatomy of the nose can be divided into the external nose and the nasal cavity. Anatomy of the Nose, mouth, and throat
  • Treatment of epistaxis:
    • Used for vasoconstriction
    • Rapid onset of action with an effect lasting 30–60 minutes
    • Mostly been replaced with other local anesthetics Local anesthetics Local anesthetics are a group of pharmacological agents that reversibly block the conduction of impulses in electrically excitable tissues. Local anesthetics are used in clinical practice to induce a state of local or regional anesthesia by blocking sodium channels and inhibiting the conduction of painful stimuli via afferent nerves. Local Anesthetics with vasoconstrictors due to abuse potential

Adverse effects

  • High risk of addiction Addiction Substance use disorders are a significant cause of morbidity and mortality, especially among adolescents and young adults. A substance-related and addictive disorder is the continued use of a substance despite harmful consequences; these include significant impairment to one's health or relationships or failure to fulfill major responsibilities at work, school, or home because of substance use. Substance-Related and Addictive Disorders/cocaine-use disorder
  • Cardiovascular: Even casual cocaine use may be associated with acute or chronic cardiovascular toxicity:
    • Potent vasoconstriction → 
      • Severe hypertension
      • MI MI MI is ischemia and death of an area of myocardial tissue due to insufficient blood flow and oxygenation, usually from thrombus formation on a ruptured atherosclerotic plaque in the epicardial arteries. Clinical presentation is most commonly with chest pain, but women and patients with diabetes may have atypical symptoms. Myocardial Infarction
      • Ischemic stroke Ischemic Stroke An ischemic stroke (also known as cerebrovascular accident) is an acute neurologic injury that occurs as a result of brain ischemia; this condition may be due to cerebral blood vessel occlusion by thrombosis or embolism, or rarely due to systemic hypoperfusion. Ischemic Stroke
    • Tachyarrhythmias due to norepinephrine reuptake inhibition
    • Enhanced thrombus formation
  • Respiratory (in cases of crack cocaine consumption and abuse):
    • Pulmonary fibrosis Pulmonary Fibrosis Idiopathic pulmonary fibrosis is a specific entity of the major idiopathic interstitial pneumonia classification of interstitial lung diseases. As implied by the name, the exact causes are poorly understood. Patients often present in the moderate to advanced stage with progressive dyspnea and nonproductive cough. Pulmonary Fibrosis
    • Pneumothorax Pneumothorax A pneumothorax is a life-threatening condition in which air collects in the pleural space, causing partial or full collapse of the lung. A pneumothorax can be traumatic or spontaneous. Patients present with a sudden onset of sharp chest pain, dyspnea, and diminished breath sounds on exam. Pneumothorax
  • GI: increased incidence of perforated ulcers
  • Pregnancy Pregnancy Pregnancy is the time period between fertilization of an oocyte and delivery of a fetus approximately 9 months later. The 1st sign of pregnancy is typically a missed menstrual period, after which, pregnancy should be confirmed clinically based on a positive β-hCG test (typically a qualitative urine test) and pelvic ultrasound. Pregnancy: Diagnosis, Maternal Physiology, and Routine Care: increased fetal morbidity and mortality; growth restriction

Other CNS Stimulants

Clinical uses

  • ADHD: 
    • Methylphenidate (Ritalin, Concerta)
    • CNS stimulant but not an amphetamine derivative
  • Obesity Obesity Obesity is a condition associated with excess body weight, specifically with the deposition of excessive adipose tissue. Obesity is considered a global epidemic. Major influences come from the western diet and sedentary lifestyles, but the exact mechanisms likely include a mixture of genetic and environmental factors. Obesity/anorexiant medications:
    • Phentermine
    • Phendimetrazine
    • Diethylpropion
  • Narcolepsy, shift work sleep Sleep Sleep is a reversible phase of diminished responsiveness, motor activity, and metabolism. This process is a complex and dynamic phenomenon, occurring in 4-5 cycles a night, and generally divided into non-rapid eye movement (NREM) sleep and REM sleep stages. Physiology of Sleep disorder, excessive daytime sleepiness:
    • Modafinil (Provigil)
    • Pitolisant (Wakix)
    • Armodafinil (Nuvigil)

References

  1. Farzam, K., Faizy, R.M., Saadabadi, A. (2021). Stimulants. StatPearls. Retrieved September 24, 2021, from http://www.ncbi.nlm.nih.gov/books/NBK539896/
  2. Giardina, E. (2021). Cardiovascular effects of caffeine and caffeinated beverages. UpToDate. Retrieved September 24, 2021, from https://www.uptodate.com/contents/cardiovascular-effects-of-caffeine-and-caffeinated-beverages
  3. Murray, A., Traylor, J. (2021). Caffeine toxicity. StatPearls. Retrieved September 24, 2021, from http://www.ncbi.nlm.nih.gov/books/NBK532910/
  4. Sandhu, A., Hosseini, S.A., Saadabadi, A. (2021). Nicotine. StatPearls. Retrieved September 24, 2021, from http://www.ncbi.nlm.nih.gov/books/NBK493148/
  5. National Center for Biotechnology Information (2021). PubChem Compound Summary for CID 3007, Amphetamine. Retrieved June 24, 2021, from https://pubchem.ncbi.nlm.nih.gov/compound/Amphetamine
  6. Butterworth, J.F., Lahaye, L. (2021). Clinical use of local anesthetics in anesthesia. UpToDate. Retrieved September 24, 2021, from https://www.uptodate.com/contents/clinical-use-of-local-anesthetics-in-anesthesia

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