Pharmacology Exam Flashcards

Flashcards generated from lecture notes for exam review.

Nicotine Content in Tobacco

Dried tobacco leaves contain approximately 5% nicotine.

Nicotine Carrier in Smoke

Tar is the substance in tobacco smoke that carries nicotine to the lungs.

US Adult Tobacco Use

About 20% of US adults are current users of tobacco products.

Fastest Nicotine Delivery

Smoking/vaporizing provides the highest blood nicotine levels.

Nicotine Travel Time

With smoking/vaping, it takes nicotine approximately 7 seconds to hit the brain.

Nicotine Metabolism and Smoking

People with reduced nicotine metabolism are more likely to become smokers.

Nicotine Receptor Action

Nicotine is an agonist at nicotinic acetylcholine receptors (nAChRs).

nAChR Receptor Type

Nicotinic acetylcholine receptors (nAChRs) are ionotropic receptors.

Nicotine and Attention

Nicotine can enhance performance of attention-demanding tasks.

Nicotine Tolerance Type

Acute tolerance to nicotine develops over the course of the day due to desensitization of nicotinic receptors (nAChRs).

Acetylcholine Precursor

Choline is the precursor for acetylcholine.

Acetylcholine Synthesis Enzyme

Choline acetyl-transferase (ChAT) is the enzyme that synthesizes acetylcholine.

Acetylcholine Metabolism Enzyme

Acetylcholinesterase (AChE) is the enzyme that metabolizes acetylcholine.

VAChT Function

Vesicular acetylcholine transporter (VAChT) packages ACh into vesicles.

Metabotropic ACh Receptors

Muscarinic ACh receptors (mAChRs) are metabotropic.

nAChR Subunit Number

Nicotinic ACh receptors (nAChRs) have 5 subunits.

nAChR Subunit Composition

Nicotinic ACh receptors can consist of 5 alpha subunits, or 2 alpha and 3 beta subunits

Muscle nAChR Binding Sites

Muscle nAChRs have 2 ACh binding sites.

nAChR Channel Type

nAChRs are cation channels.

Nicotine's Effect on Dopamine

Nicotine increases firing activity of dopamine cells in the VTA and increases dopamine release at terminals in the nucleus accumbens.

Rewarding Nicotine Receptor

Alpha4-beta2-containing receptors are involved in the rewarding effects of nicotine.

Cognitive Nicotine Receptor

Alpha7-containing receptors are involved in the cognitive effects of nicotine.

Alpha7 Knockout Impact

IV nicotine self-administration will not be impaired if you knockout the alpha7-containing nAChRs in mutant mice.

Menthol for Nicotine Addiction

Menthol is not used to treat nicotine addiction.

Nicotine Treatment Options

Nicotine replacement therapy helps with nicotine dependence/withdrawal, while buproprion and varenicline target dependence/withdrawal AND cravings.

Opiate Definition

Opiates are naturally-occurring alkaloids found in the sap of the opium poppy.

Opioid Overdose Effects

At high doses, opioids can lead to coma and death.

Opium Ingredients

Morphine and codeine are the principal active ingredients in opium.

Heroin Formation

Heroin is formed by adding two acetyl groups to morphine, thus increasing lipid solubility.

Fentanyl Potency

Fentanyl is 8-10x more potent than morphine.

Opioid Medical Uses

Medical uses of prescription opioids include cough suppression, and severe pain relief.

OxyContin's Role

Purdue aggressively marketing OxyContin greatly contributed to the prescription opioid and heroin epidemic.

Opioid Addiction Rate

Approximately 15% of people who are prescribed opioids for pain management become addicted.

Opioid Administration Routes

Recreational routes of administration for opioids include IV injection, SC injection, smoking/inhalation, and snorting.

Methadone Half Life

Methadone has a half life of 24 hours due to depot binding.

Low to Moderate Opioid Effects

Opioid effects at low to moderate doses include pinpoint pupils and reduced GI motility (constipation).

High Dose Opioid Effects

Opioid effects at high doses include pinpoint pupils.

Endogenous Opioid Type

All endogenous opioids are peptide neurotransmitters.

Endogenous Opioid Roles

Endogenous opioids can act as both neurotransmitters and hormones.

Abused Opioid Receptor

All abused opioids bind to the mu opioid receptor.

Opioid Receptor Type

Opioid receptors are metabotropic.

Opioid Receptor Location

Opioid receptors can be pre or post synaptic.

Prescription Opioid Action

Many prescription and abused opioid drugs are opioid agonists.

Opioid Antagonists

Naloxone and naltrexone are opioid competitive antagonists.

Buprenorphine Action

Buprenorphine is an opioid partial agonist.

MOR Knockout Impact

Genetic knockout of the mu-opioid receptor (MOR) causes loss of morphine effects.

Analgesia Location

Analgesia occurs due to opioid drugs acting at the spinal cord, periaqueductal gray, and forebrain.

Rewarding Effects Location

Rewarding effects occur due to opioid drugs acting at the brain (dopamine neurons).

Respiratory Depression Location

Respiratory Depression occurs due to opioid drugs acting at the brainstem.

Gastrointestinal Effects Location

Gastrointestinal effects occur due to opioid drugs acting at the stomach, small intestine, and large intestine.

Nausea/Vomiting Location

Nausea/vomiting occurs due to opioid drugs acting at the area postrema, vestibular system, and GI tract.

Cough Suppression Location

Cough suppression occurs due to opioid drugs acting at the brainstem.

Pupil Constriction Location

Pupil constriction occurs due to opioid drugs acting at the brainstem.

Dopamine and Morphine CPP

Dopamine deficient mice do not show morphine conditioned place preference.

Loperamide Function

Loperamide (Imodium) is a modified opioid that acts peripherally and is used to slow GI motility and reduce diarrhea.

Dextromethorphan's Origin

Dextromethorphan was developed as a non-addictive substitute for codeine.

Primary Psychoactive Cannabinoid

Delta9-tetrahydrocannabinol is the most important psychoactive compound in cannabis.

THC Content Trend

THC content in seized marijuana has increased over the decades.

Hashish Definition

Hashish is a dried resin concentration consisting of trichomes.

THC Absorption via Smoking

Smoking allows for 20-30% of the THC to be absorbed.

Cannabis Popularity

Cannabis is currently the most popular illicit drug in the US.

Medical uses of Cannabis

Potential medical uses of cannabis include analgesia, antiemetic effects, and anticonvulsant effects.

FDA approved use for CBD

CBD medication is approved in the US for severe childhood epilepsy.

THC depot binding effects

Depot binding of THC does not cause a rapid increase in peak blood concentration.

THC Half Life

The half life of THC is 20-30 hours.

Active THC Metabolite

11-hydroxy-THC is the ACTIVE metabolic product after oral consumption of delta9-THC (first pass metabolism).

Inactive THC Metabolite

11-nor-9-carboxy-THC is the INACTIVE metabolic product of THC that's detected in blood tests.

THC Lethality

THC is non-lethal at extremely high doses.

THC Tolerance Mechanism

Pharmacodynamic tolerance after repeated marijuana use occurs due to desensitization and downregulation of CB1 receptors in the brain.

Spice and K2 Schedule

Spice and K2 are placed on the schedule 1 list.

CB1 Receptor Location

CB1 cannabinoid receptors are located on presynaptic terminals for retrograde signaling.

Endocannabinoid Solubility

Endogenous cannabinoids all have high lipid solubility.

2-AG Receptor Action

2-AG (an endocannabinoid) is a full agonist for both CB1 and CB2 receptors.

Anandamide Receptor Action

Anandamide (an endocannabinoid) is a partial agonist for CB1 receptors.

Endocannabinoid Type

Endocannabinoids are lipid neurotransmitters.

Endocannabinoid Storage

Endocannabinoids are not stored in vesicles.

Endocannabinoid Travel

Endocannabinoids travel retrogradely to the pre-synaptic terminal and bind to CB1 receptors.

Cannabinoid Receptor Type

The two known cannabinoid receptors are both metabotropic.

CB1 and CB2 Location

CB1 receptors are expressed mostly in the brain and spinal cord, and CB2 receptors are expressed mostly in the immune system.

CB1 Receptor Role

The CB1 receptor is important for the rewarding effects and "high" from cannabis.

CB1 Receptor Action

The Gi protein coupled to the CB1 receptor acts to reduce activity of voltage-gated calcium channels.

THC Self-Administration

High doses of THC are not self-administered by animals.

Low Dose THC CPP

Low doses of THC show conditioned place preference.

CB1 Agonists Effect on Dopamine

CB1 agonists increase dopamine firing in the VTA and dopamine release in the nucleus accumbens.

Cannabinoids reward

Cannabinoids injected IV or into the nucleus accumbens cause pleasurable reactions to tastes.

Cannabinoids Memory

Cannabinoids injected IV or into the hippocampus cause deficits in working memory.

CB1 Knockout Effect

CB1 knockout mice show impaired extinction learning.

Cannabis Addiction

Cannabis use can lead to addiction.

Cannabis lung Problems

Long term cannabis use can lead to long-term lung problems.

Cannabis IQ Reduction

There is evidence of reduced IQ following weekly use of cannabis in adolescence.

Psychedelics

Classical psychedelics (serotonergic agonists) include LSD, DMT, Mescaline, and Psilocybin.

Hallucinogen Types Effects

Psychedelics cause Hallucinations, altered state of consciousness, Dissociatives cause Distorted perceptions, feelings of detachment from self & environment, and Deliriants cause State of stupor, confusion, and distorted memory.

Indolamine Psychedelic Similarity

Indolamine psychedelics (tryptamines) are structurally similar to serotonin.

Phenethylamine Source

Mescaline is the natural source of phenethylamine psychedelics.

Indolamine Synthetic Source

LSD is the synthetic source of indolamine psychedelics.

Ayahuasca's Composition

Ayahuasca is a drink that comes from 2 plants to provide DMT and beta-carboline.

LSD Origin

LSD is a synthetic compound.

Mescaline Source

Mescaline is found in several species of cactus, including the peyote cactus.

First LSD Trip

Albert Hofmann experienced the first LSD "trip".

Smoked DMT Duration

Smoked DMT has an onset of within seconds and a duration of only 30-60 seconds.