44 Pharmacology – 2
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1. The use of ethanol in methanol poisoning is an example of competitive agonism. | ![]() |
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2. Compliance therapy has been shown to improve the outcome in patients prescribed neuroleptic medication. | ![]() |
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3. Zero-order kinetics can be correctly described in terms of half-life. | ![]() |
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4. Heteroceptors regulate neurotransmitter release. | ![]() |
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5. Heteroceptors can be ionotropic or metabotropic. | ![]() |
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6. Acetylcholine is a transmitter at some postganglionic sympathetic neuroeffector junctions. | ![]() |
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7. Muscarinic receptors are coupled to ion channels. | ![]() |
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8. Pregabalin binds to the alpha 2 delta subunit of voltage-sensitive calcium channels. | ![]() |
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9. DHEA has an effect opposite to that of cortisol. | ![]() |
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10. Benzhexol inhibits dopamine secretion. | ![]() |
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11. The firing rate of neurons in the mesolimbic pathway changes in anticipation of pleasurable stimuli. | ![]() |
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12. Dopamine receptors are postsynaptic but not presynaptic. | ![]() |
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13. Raclopride is used to study dopamine receptor binding. | ![]() |
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14. Opiates regulate dopamine activity. | ![]() |
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15. Glutamate concentration is increased in post-mortems of schizophrenic brains. | ![]() |
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16. Magnesium ions block NMDA receptors. | ![]() |
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17. Nicotine reaches the brain within 5–6 seconds after inhalation. | ![]() |
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18. Nicotine increases the brain dopamine in the mesolimbic region. | ![]() |
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19. The NMDA receptor is a voltage gated channel. | ![]() |
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20. β-adrenergic receptors are stimulatory. | ![]() |
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21. The upper limit for a normal QT interval is approximately 400 ms. | ![]() |
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22. Increased 5-HT in the periaqueductal grey matter increases the fright/flight response. | ![]() |
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23. Serotonin transporter gene polymorphisms are associated with violence. | ![]() |
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24. In neuroimaging, iodobenzamide may be used as a ligand for 5-HT2A receptors. | ![]() |
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25. Yohimbine is an α2-noradrenergic receptor antagonist. | ![]() |
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ANSWERS
False: Ethanol competes for occupancy of the enzyme alcohol dehydrogenase, and thus prevents the metabolism of methanol to its toxic metabolite formic acid. This is an example of competitive antagonism (Bennett & Brown 2003, p. 92; King 2004, p. 76).
False: In zero-order kinetics the rate of the metabolism or elimination is not related to the concentration of the drug, but occurs at a constant rate, e.g. the metabolism of alcohol. First-order kinetics can be described in terms of half-life (Anderson & Reid 2002, p. 28; Bennett & Brown 2003, p. 99).
True: Neurotransmitter receptors are usually located on a membrane on the far side of the synapse to the point of release. When these postsynaptic receptors are located on the dendrites or the soma of a neuron they regulate cell firing. When located on a nerve terminal and regulating neurotransmitter release they are called presynaptic heteroceptors. Presynaptic heteroceptors regulate neurotransmitter release by the axon terminal on which they are located. For example, mirtazapine blocks α2-heteroceptors on serotonergic neurons, resulting in increased serotonin release (Anderson & Reid 2002, p. 10).
True: Ionotropic receptors are ligand-gated ion channels that respond to neurotransmitters by allowing ion flux across cell membranes. Metabotropic receptors, however, mediate neurotransmission less directly by activating second messenger molecules which subsequently modulate cellular communication (Rang et al 2003, p. 22).
True: The sympathetic transmitter at the postganglionic synapse is usually noradrenaline, but in sweat glands and in some blood vessels it is acetylcholine. The postganglionic parasympathetic neurotransmitter is acetylcholine (Rang et al 2003, p. 123).
False: Muscarinic receptors are G-protein coupled (Anderson & Reid 2002, p. 22).
True: DHEA can act as an anti-glucocorticoid (Goodyer et al 2003).
True: Anticholinergic drugs exert an excitatory effect, opposite to that of dopamine, on striatal neurons. They also exert a presynaptic inhibitory effect on dopaminergic nerve terminals and hence inhibit dopamine secretion (Rang et al 2003, p. 500).
True: The dopamine firing rate changes during the anticipation and possibly also during the experience of pleasurable or dreaded stimuli. This pathway is strongly associated with motivation, reward behaviour and dependence on drugs of abuse (Anderson & Reid 2002, p. 12; Sadock & Sadock 2005, p. 1393).
False: Dopamine receptors can be pre- or postsynaptic. Postsynaptic dopamine receptors are located on the far side of the synapse to the point of release. The presynaptic receptors are located on the dopamine neurons and are called autoreceptors. Stimulation of these autoreceptors inhibits the release of dopamine by the neuron. The D2 receptors are located post- as well as presynaptically (Anderson & Reid 2002, p. 10; Cooper et al 2003, p. 240).
True: Raclopride is a D2 receptor antagonist. Other compounds used to image dopamine receptors include other benzamides such as iodobenzamide and fallypride, and butyrophenones such as spiperone/spiroperidol derivatives (King 2004, p. 24).
False: Post-mortem studies in schizophrenic brains show reduced concentrations of glutamate in the hippocampus and the prefrontal cortex. This suggests that there is decreased glutaminergic transmission in schizophrenia (Sadock & Sadock 2005, p. 70).
True: Magnesium readily blocks NMDA receptors. This block shows marked voltage dependence, occurring at physiological magnesium concentrations when the cell is normally polarized, but is overcome if the cell is depolarized (Kandel et al 2000, p. 212; Rang et al 2003, p. 466).
True: Nicotine is absorbed through the skin, mucous membranes and lungs. With smoking, nicotine is rapidly absorbed across the lung mucosa and produces effects on the brain within about 7 seconds (King 2004, p. 507).
True: The mesolimbic dopaminergic pathway that projects from the ventral tegmental area to the nucleus accumbens is strongly associated with motivation, reward behaviour and dependence on drugs of abuse. The stimulant and rewarding effects of nicotine are mediated via the nicotinic cholinergic receptors that indirectly increase the release of dopamine from the nucleus accumbens (Anderson & Reid 2002, p. 12; King 2004, p. 506; Sadock & Sadock 2005, p. 1393).
False: The NMDA receptor is a ligand-gated ion channel, activated by glutamate. The NMDA receptor is unique among transmitter-gated channels because its opening also depends on membrane voltage (which will expel Mg2+ from the channel by electrostatic repulsion, allowing Ca2+ and Na+ to enter). Thus it is sensitive to voltage. It controls a cation channel that is permeable to Ca2+ as well as to Na+ and K+ (Cooper et al 2003, p. 139; Kandel et al 2000, p. 212).
True: β-adrenoceptors are stimulatory. Their stimulation increases cAMP (Anderson & Reid 2002, p. 16).
False: The QT interval is the time in milliseconds between the beginning of the QRS complex and the end of the T wave. Prolongation is associated with ventricular arrhythmias and sudden death. QT is dependent on heart rate. The Bazett’s formula (QT/√RR interval) is applied to give a QT corrected for rate (QTc). Normal QTc is <450 ms in women and <430 ms in men. Prolonged values are >470 ms in women and >450 ms in men (King 2004, p. 581).
True: Transporters or monoamine plasma membrane transported proteins mediate the reuptake of monoamines released into the synaptic cleft back into the presynaptic terminal. There is an inverse association between 5-HT and impulsivity, aggression and violence (Johnstone et al 2004, p. 509; Sadock & Sadock 2005, p. 54).
True: Yohimbine is an α2 antagonist which increases noradrenaline release. It precipitates panic attacks in patients with panic disorder, but not in healthy volunteers. It was considered an aphrodisiac. It sometimes helps in psychogenic impotence (Anderson & Reid 2002, p. 96; King 2004, p. 560).