Evidence review and clinical guidance for the use of ziprasidone in Canada

David M Gardner; Andrea L Murphy; Stan Kutcher; Serge Beaulieu; Carlo Carandang; Alain Labelle; Pierre Lalonde; Ashok Malla; Heather Milliken; Claire O’Donovan; Ayal Schaffer; Jorge Soni; Valerie H Taylor; Richard Williams

doi:10.1186/1744-859X-12-1

Annals of General Psychiatry

Table 1 Antipsychotic affinities ( K_i) and target daily dosing range in schizophrenia [7, 9–11]

From: Evidence review and clinical guidance for the use of ziprasidone in Canada

Antipsychotic	Very high	High	Moderate	Low	Negligible
daily dose	(K_i < 1.0)	(K_i 1.0–9.9)	(K_i 10–99)	(K_i 100–999)	(K_i ≥1000)
Ziprasidone	5HT_{2a (0.4)}	5HT_{1a (2.5) **}	α_{1 (13)}	D_{1 (130)}	M_{1 (5100)}
120-160 mg	5HT_{2c (0.7)}	D_{2 (3.1)}	D_{4 (32)}	α_{2 (310)}
		D_{3 (7.2)}	H_{1 (47)}
		5HT_{7 (9.3)}	NA_{uptake (48)}
			5HT_{uptake (53)}
			5HT_{6 (76)}
Aripiprazole	D₂_{(0.3) **}	5HT_{1a (1.7) **}	D_{4 (44)}		M_{1 (>1000)}
15-30 mg	D₃_(0.8)	5HT_2a_(3.4)	5HT_{2c (15)}
			5HT_{7 (39)}
			α_{1 (57)}
			H_{1 (61)}
			5HT_{uptake (98)}
Risperidone	5HT_2a_(0.3)	α_{1 (1.4)}	5HT_{2c (10)}	5HT_1A₍₂₁₀₎	5HT_{uptake (1400)}
4-6 mg		D_{2 (2.2)}	H_{1 (19)}	D₁₍₅₈₀₎	5HT_{6 (2000)}
		5HT_{7 (3.0)}			M_{1 (2800)}
		D_{3 (9.6)}			NA_{uptake (28,000)}
		D_{4 (8.5)}
		α_{2 (5.1)}
Paliperidone		5HT_2a_(1.0)	α_{2 (17)}	5HT_1A₍₅₉₀₎	M_{1 (3570)}
6-9 mg		5HT_{7 (1.3)}	H_{1 (32)}	D₁₍₆₇₀₎
		α_{1 (4.0)}	D_{4 (30)}
		D_{2 (4.8)}	5HT_{2c (71)}
		D_{3 (6.9)}
Olanzapine		H₁_(2.8)	5HT_{2c (10)}	α_{2 (170)}	5HT_{1a (2100)}
10-20 mg		5HT_2a_(3.3)	5HT_{6 (10)}	5HT_{7 (250)}	NA_{uptake (2000)}
		M₁_(4.7)	D_{2 (20)}		5HT_{uptake (>15,000)}
			D_{3 (45)}
			D_{1 (52)}
			α_{1 (54)}
			D_{4 (60)}
Clozapine		H₁_(1.8)	5HT_{6 (11)}	D_{4 (54)}	5HT_{uptake (3900)}
200-500 mg		M₁_(1.8)	5HT_{2c (17)}	D_{2 (130)}
		α_{1 (4.0)}	α_{2 (33)}	5HT_{1a (140) **}
		5HT_{2a (8.9)}	5HT_{7 (66)}	D_{3 (240)}
				D_{1 (290)}
				NA_{uptake (390) *}
Quetiapine		H_{1 (8.7)}	α_{1 (15)}	M_{1 (100)}	α_{2 (1000)}
400-800 mg				D_{2 (180)}	D_{1 (1300)}
				5HT_{2a (220)}	5HT_{2c (1400)}
				5HT_{1a (230) **}	5HT_{7 (1800)}
				D_{3 (320)}	D_{4 (2200)}
				NA_{uptake (680)*}	5HT_{6 (4100)}
					5HT_{uptake (>18,000)}

* Quetiapine’s active metabolite N-desalkyl-quetiapine inhibits NA uptake (35 nM). Clozapine’s active metabolite N-desmethyl-clozapine also has a low affinity for NA uptake inhibition.
** Partial agonist. Quetiapine’s active metabolite N-desalkyl-quetiapine is a 5HT_1a partial agonist (191 nM). Clozapine’s active metabolite N-desmethyl-clozapine is a 5HT_1a partial agonist (105 nM).
5-HT: serotonin; D: dopamine; H: histamine; M: muscarinic cholinergic; α: alpha-adrenergic.
Lower values (shown in parentheses) indicate higher affinities at receptors or greater inhibition of pre-synaptic neurotransmitter uptake. Antipsychotics used in relatively small daily doses are unlikely to have clinical effects at receptors for which they have low affinity, unlike antipsychotics used at high daily doses.

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ISSN: 1744-859X

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